Lennart Bunch
Professor
Medicinal Chemistry
Jagtvej 162
2100 København Ø
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(S)-2-Mercaptohistidine: A First Selective Orthosteric GluK3 Antagonist
Poulie, Christian Bernard Matthijs, Larsen, Y., Leteneur, C., Barthet, G., Bjørn-Yoshimoto, Walden, Malhaire, F., Nielsen, Birgitte, Pin, J. P., Mulle, C., Pickering, Darryl S & Bunch, Lennart, 2022, In: ACS Chemical Neuroscience. 13, 10, p. 1580–1587Research output: Contribution to journal › Journal article › Research › peer-review
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4,4-Dimethyl- and diastereomeric 4-hydroxy-4-methyl-(2S)-glutamate analogues display distinct pharmacological profiles at ionotropic glutamate receptors and excitatory amino acid transporters
Bunch, Lennart, Pickering, Darryl S, Gefflaut, T., Vinatier, V., Helaine, V., Amir, A., Nielsen, Birgitte & Jensen, Anders A., 2009, In: ChemMedChem. 4, 11, p. 1925-1929Research output: Contribution to journal › Journal article › Research › peer-review
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Beta-Sulfonamido Functionalized Aspartate Analogs as Excitatory Amino Acid Transporter Inhibitors: Distinct Subtype-Selectivity Profiles Arising from Subtle Structural Differences
Hansen, J. C., Bjørn-Yoshimoto, Walden, Bisballe, N., Nielsen, Birgitte, Jensen, Anders A. & Bunch, Lennart, 2016, In: Journal of Medicinal Chemistry. 59, p. 8771-8786 16 p.Research output: Contribution to journal › Journal article › Research › peer-review
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A Diversity Oriented Synthesis Approach to New 2,3-trans-Substituted l-Proline Analogs as Potential Ligands for the Ionotropic Glutamate Receptors
Kayser, S., Temperini, Piero, Poulie, Christian Bernard Matthijs, Staudt, Markus, Nielsen, Birgitte, Pickering, Darryl S & Bunch, Lennart, 4 Mar 2020, In: ACS Chemical Neuroscience. 11, p. 702-714 13 p.Research output: Contribution to journal › Journal article › Research › peer-review
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A General and Convenient Method for the Rhodium-Catalysed Decarbonylation of Aldehydes
Kreis, M., Palmelund, A., Bunch, Lennart & Madsen, R., 2006, In: Advanced Synthesis & Catalysis. 348, 15, p. 2148-2154Research output: Contribution to journal › Journal article › Research › peer-review
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A multifaceted GABAA receptor modulator: Functional properties and mechanism of action of the sedative-hypnotic and recreational drug methaqualone (Quaalude)
Hammer, H., Bader, B. M., Ehnert, C., Bundgaard, C., Bunch, Lennart, Hoestgaard-Jensen, K., Schroeder, O. H., Bastlund, J. F., Gramowski-Voß, A. & Jensen, Anders A., 2015, In: Molecular Pharmacology. 88, 2, p. 401-420 20 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Allosteric modulation of an excitatory amino acid transporter: The subtype-selective inhibitor UCPH-101 exerts sustained inhibition of EAAT1 through an intramonomeric site in the trimerization domain
Abrahamsen, B., Schneider, N., Erichsen, M. N., Huynh, Tri Hien Viet, Fahlke, C., Bunch, Lennart & Jensen, Anders A., 2013, In: Journal of Neuroscience. 33, 3, p. 1068-1087Research output: Contribution to journal › Journal article › Research › peer-review
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Augmentation of Anticancer Drug Efficacy in Murine Hepatocellular Carcinoma Cells by a Peripherally Acting Competitive N-Methyl-d-aspartate (NMDA) Receptor Antagonist
Gynther, M., Proietti Silvestri, I., Hansen, J. C., Hansen, K. B., Malm, T., Ishchenko, Y., Larsen, Y., Han, L., Kayser, S., Auriola, S., Petsalo, A., Nielsen, Birgitte, Pickering, Darryl S & Bunch, Lennart, 14 Dec 2017, In: Journal of Medicinal Chemistry. 60, 23, p. 9885-9904 20 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Azetidinic amino acids: stereocontrolled synthesis and pharmacological characterization as ligands for glutamate receptors and transporters
Bräuner, Hans, Bunch, Lennart, Chopin, N., Couty, F., Evano, G., Jensen, Anders A., Kusk, M. L., Nielsen, Birgitte & Rabasso, N., 2005, In: Organic & Biomolecular Chemistry. 3, 21, p. 3926-36 11 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Benzoxazoles and oxazolopyridines in medicinal chemistry studies
Demmer, C. S. & Bunch, Lennart, 2015, In: European Journal of Medicinal Chemistry. 97, p. 778-785 8 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Binding Mode of an α-Amino Acid-Linked Quinoxaline-2,3-dione Analogue at Glutamate Receptor Subtype GluK1
Demmer, C. S., Møller, C., Brown, P. M. G. E., Han, L., Pickering, Darryl S, Nielsen, Birgitte, Bowie, D., Frydenvang, Karla Andrea, Kastrup, Jette Sandholm Jensen & Bunch, Lennart, 9 Apr 2015, In: A C S Chemical Neuroscience. 6, p. 845-854 10 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Binding site and interlobe interactions of the ionotropic glutamate receptor GluK3 ligand binding domain revealed by high resolution crystal structure in complex with (S)-glutamate
Venskutonyte, R., Frydenvang, Karla Andrea, Gajhede, Michael, Bunch, Lennart, Pickering, Darryl S & Kastrup, Jette Sandholm Jensen, Dec 2011, In: Journal of Structural Biology. 176, 3, p. 307-314Research output: Contribution to journal › Journal article › Research › peer-review
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Bioavailability studies and in vitro profiling of selective excitatory amino acid transporter subtype 1 (EAAT1) inhibitor 2-amino-4-(4-methyl)-7-(naphthalen-1-yl)-5-oxo-5,6,7,8-tetrahydro-4H-chromene-3-carbonitrile (UCPH-102)
Haym, I., Huynh, Tri Hien Viet, Hansen, S. W., Pedersen, M. H. F., Ruiz, J. A., Erichsen, M. N., Gynther, M., Bjørn-Yoshimoto, Walden, Abrahamsen, B., Bastlund, J. F., Bundgaard, C., Eriksen, A. L., Jensen, Anders A. & Bunch, Lennart, 2016, In: ChemMedChem. 11, 4, p. 403-419 17 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Blood-brain barrier permeability and brain uptake mechanism of kainic Acid and dihydrokainic Acid
Gynther, M., Petsalo, A., Hansen, S. H., Bunch, Lennart & Pickering, Darryl S, Mar 2015, In: Neurochemical Research. 40, 3, p. 542-549 8 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Chemo-enzymatic synthesis of (2S,4R)-2-amino-4-(3-(2,2-diphenylethylamino)-3-oxopropyl)pentanedioic acid: a novel selective inhibitor of human excitatory amino acid transporter subtype 2
Sagot, E., Jensen, Anders A., Pickering, Darryl S, Pu, X., Umberti, M., Stensbøl, T. B., Nielsen, Birgitte, Assaf, Z., Aboab, B., Bolte, J., Gefflaut, T. & Bunch, Lennart, 2008, In: Journal of Medicinal Chemistry. 51, 14, p. 4085-4092 8 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Chemo-enzymatic synthesis of a series of 2,4-syn-functionalized (S)-glutamate analogues: new insight into the structure-activity relation of ionotropic glutamate receptor subtypes 5, 6, and 7.
Sagot, E., Pickering, Darryl S, Pu, X., Umberti, M., Stensbøl, T. B., Nielsen, Birgitte, Chapelet, M., Bolte, J., Gefflaut, T. & Bunch, Lennart, 2008, In: Journal of Medicinal Chemistry. 51, 14, p. 4093-103Research output: Contribution to journal › Journal article › Research › peer-review
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Chemo-enzymatic synthesis of new 2,4-syn-functionalized (S)-glutamate analogues and structure-activity relationship studies at ionotropic glutamate receptors and excitatory amino acid transporters
Assaf, Z., Larsen, A. P., Venskutonyte, R., Han, L., Abrahamsen, B., Nielsen, Birgitte, Gajhede, Michael, Kastrup, Jette Sandholm Jensen, Jensen, Anders A., Pickering, Darryl S, Frydenvang, Karla Andrea, Gefflaut, T. & Bunch, Lennart, 2013, In: Journal of Medicinal Chemistry. 56, 4, p. 1614-1628Research output: Contribution to journal › Journal article › Research › peer-review
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Chemoenzymatic synthesis and pharmacological characterization of functionalized aspartate analogues as novel excitatory amino acid transporter inhibitors
Fu, H., Zhang, J., Tepper, P. G., Bunch, Lennart, Jensen, Anders A. & Poelarends, G. J., 13 Sep 2018, In: Journal of Medicinal Chemistry. 61, 17, p. 7741-7753Research output: Contribution to journal › Journal article › Research › peer-review
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Chemoenzymatic synthesis of a series of 4-substituted glutamate analogues and pharmacological characterization at human glutamate transporters subtypes 1-3
Alaux, S., Kusk, M., Sagot, E., Bolte, J., Jensen, Anders A., Bräuner, Hans, Gefflaut, T. & Bunch, Lennart, 2005, In: Journal of Medicinal Chemistry. 48, 25, p. 7980-92 13 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Convenient access to β-substituted cysteines and β- and γ-mercapto prolines
Hansen, J. C., Rabuffetti, M. & Bunch, Lennart, 2023, In: Canadian Journal of Chemistry. 101, 5, p. 326-333Research output: Contribution to journal › Journal article › Research › peer-review
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Corrigendum to "Binding site and interlobe interactions of the ionotropic glutamate receptor GluK3 ligand binding domain revealed by high resolution crystal structure in complex with (S)-glutamate" [J. Struct. Biol. 176 (2011) 307-314]
Venskutonyte, R., Frydenvang, Karla Andrea, Gajhede, Michael, Bunch, Lennart, Pickering, Darryl S & Kastrup, Jette Sandholm Jensen, Nov 2013, In: Journal of Structural Biology. 184, 2, p. 381 1 p.Research output: Contribution to journal › Comment/debate › Research › peer-review
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Delineation of the functional properties and the mechanism of action of AA29504, an allosteric agonist and positive allosteric modulator of GABAA receptors
Olander, E. R., Madjroh, Nawid, Bunch, Lennart, Söderhielm, P. C. & Jensen, Anders A., 2018, In: Biochemical Pharmacology. 150, p. 305-319Research output: Contribution to journal › Journal article › Research › peer-review
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Derivatives of (R)-3-(5-Furanyl)carboxamido-2-aminopropanoic Acid as Potent NMDA Receptor Glycine Site Agonists with GluN2 Subunit-Specific Activity
Zhao, F., Atxabal, U., Mariottini, S., Yi, F., Lotti, J. S., Rouzbeh, N., Liu, N., Bunch, Lennart, Hansen, K. B. & Clausen, Rasmus Prætorius, 2022, In: Journal of Medicinal Chemistry. 65, 1, p. 734-746Research output: Contribution to journal › Journal article › Research › peer-review
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Design and Synthesis of 2,3-trans-Proline Analogs as Ligands for the Ionotropic Glutamate Receptors and the Excitatory Amino Acid Transporters
Poulie, Christian Bernard Matthijs, Alcaide Lopez, A., Krell-Jørgensen, M. P., Larsen, Y., Astier, E., Bjørn-Yoshimoto, Walden, Yi, F., Syrenne, J. T., Storgaard, M., Nielsen, Birgitte, Frydenvang, Karla Andrea, Jensen, Anders A., Hansen, K. B., Pickering, Darryl S & Bunch, Lennart, 19 Jun 2019, In: A C S Chemical Neuroscience. 10, 6, p. 2989-3007 19 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Design and Synthesis of a Series of L-trans-4-Substituted Prolines as Selective Antagonists for the Ionotropic Glutamate Receptors Including Functional and X-ray Crystallographic Studies of New Subtype Selective Kainic Acid Receptor Subtype 1 (GluK1) Antagonist (2S,4R)-4-(2-Carboxyphenoxy)pyrrolidine-2-carboxylic Acid
Krogsgaard-Larsen, N., Delgar, C., Koch, K., Brown, P. M. G. E., Møller, C., Han, L., Huynh, Tri Hien Viet, Hansen, S. W., Nielsen, Birgitte, Bowie, D., Pickering, Darryl S, Kastrup, Jette Sandholm Jensen, Frydenvang, Karla Andrea & Bunch, Lennart, 2017, In: Journal of Medicinal Chemistry. 60, 1, p. 441-457 17 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Design, Synthesis, Pharmacology, and In Silico Studies of (1S,2S,3S)-2-((S)-Amino(carboxy)methyl)-3-(carboxymethyl)cyclopropane-1-carboxylic Acid (LBG30300): A Picomolar Potency Subtype-Selective mGlu2 Receptor Agonist
Liu, N., Eshak, F., Malhaire, F., Brabet, I., Prézeau, L., Renard, E., Pin, J. P., Acher, F. C., Staudt, Markus & Bunch, Lennart, 2024, In: Journal of Medicinal Chemistry. 67, 2, p. 1314–1326Research output: Contribution to journal › Journal article › Research › peer-review
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Design, Synthesis, and Pharmacological Characterization of Heterobivalent Ligands for the Putative 5-HT2A/mGlu2 Receptor Complex
Poulie, Christian Bernard Matthijs, Liu, N., Jensen, Anders A. & Bunch, Lennart, 2020, In: Journal of Medicinal Chemistry. 63, 17, p. 9928-9949 22 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Design, synthesis and pharmacological characterization of coumarin-based fluorescent analogs of excitatory amino acid transporter subtype 1 selective inhibitors, UCPH-101 and UCPH-102
Huynh, Tri Hien Viet, Abrahamsen, B., Madsen, K. K., Gonzalez-Franquesa, A., Jensen, Anders A. & Bunch, Lennart, 2012, In: Bioorganic & Medicinal Chemistry. 20, 23, p. 6831-6839Research output: Contribution to journal › Journal article › Research › peer-review
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Discovery of (R)-2-amino-3-triazolpropanoic acid derivatives as NMDA receptor glycine site agonists with GluN2 subunit-specific activity
Zhao, F., Mazis, G., Yi, F., Lotti, J. S., Layeux, M. S., Schultz, E. P., Bunch, Lennart, Hansen, K. B. & Clausen, Rasmus Prætorius, 2022, In: Frontiers in Chemistry. 10, 13 p., 1008233.Research output: Contribution to journal › Journal article › Research › peer-review
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Discovery of a New Class of Ionotropic Glutamate Receptor Antagonists by the Rational Design of (2S,3R)-3-(3-Carboxyphenyl)-pyrrolidine-2-carboxylic Acid
Larsen, A. M., Venskutonyte, R., Valadés, E. A., Nielsen, Birgitte, Pickering, Darryl S & Bunch, Lennart, 4 Nov 2011, In: ACS Chemical Neuroscience. 2, 2, p. 107-114 8 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Discovery of the first selective inhibitor of excitatory amino acid transporter subtype 1
Jensen, Anders A., Erichsen, M. N., Nielsen, C. W., Stensbøl, T. B., Kehler, J. & Bunch, Lennart, 2009, In: Journal of Medicinal Chemistry. 52, 4, p. 912-915Research output: Contribution to journal › Journal article › Research › peer-review
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Erratum: Chemoenzymatic synthesis of new 2,4- syn -functionalized (S)-glutamate analogues and structure-activity relationship studies at ionotropic glutamate receptors and excitatory amino acid transporters (Journal of Medicinal Chemistry (2013) 56 (1614-1628))
Assaf, Z., Larsen, A. P., Venskutonyteì, R., Han, L., Abrahamsen, B., Nielsen, Birgitte, Gajhede, Michael, Kastrup, Jette Sandholm Jensen, Jensen, A. A., Pickering, Darryl S, Frydenvang, Karla Andrea, Gefflaut, T. & Bunch, Lennart, 25 Jul 2013, In: Journal of Medicinal Chemistry. 56, 14, p. 5985 1 p.Research output: Contribution to journal › Comment/debate › Research › peer-review
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Excitatory amino acid transporters as potential drug targets
Bunch, Lennart, Erichsen, M. N. & Jensen, Anders A., 2009, In: Expert Opinion On Therapeutic Targets. 13, 6, p. 719-731Research output: Contribution to journal › Journal article › Research › peer-review
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Excitatory amino acid transporters: recent insights into molecular mechanisms, novel modes of modulation and new therapeutic possibilities
Jensen, Anders A., Fahlke, C., Bjørn-Yoshimoto, Walden & Bunch, Lennart, 2015, In: Current Opinion in Pharmacology. 20, p. 116-123 8 p.Research output: Contribution to journal › Journal article › Research › peer-review
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From Methaqualone and Beyond: Structure-Activity Relationship of 6-, 7-, and 8-Substituted 2,3-Diphenyl-quinazolin-4(3H)-ones and in Silico Prediction of Putative Binding Modes of Quinazolin-4(3H)-ones as Positive Allosteric Modulators of GABAA Receptors
Wang, P., Jensen, Anders A. & Bunch, Lennart, 2020, In: ACS Chemical Neuroscience. 11, 24, p. 4362-4375Research output: Contribution to journal › Journal article › Research › peer-review
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Functionalization of Oxazolo[4,5-b]pyrazines by Deprotometallation
Bisballe, N., Hedidi, M., Demmer, C. S., Chevallier, F., Roisnel, T., Dorcet, V., Halauko, Y. S., Ivashkevich, O. A., Matulis, V. E., Bentabed-Ababsa, G., Bunch, Lennart & Mongin, F., 7 Aug 2018, In: European Journal of Organic Chemistry. 29, p. 3904-3913Research output: Contribution to journal › Journal article › Research › peer-review
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Glutamate receptor agonists: stereochemical aspects
Vogensen, S. B., Greenwood, J. R., Bunch, Lennart & Clausen, Rasmus Prætorius, Apr 2011, In: Current Topics in Medicinal Chemistry. 11, 7, p. 887-906Research output: Contribution to journal › Review › Research › peer-review
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Gram-scale solution-phase synthesis of selective sodium bicarbonate Co-transport Inhibitor S0859: in vitro efficacy studies in breast cancer cells
Larsen, A. M., Krogsgaard-Larsen, N., Lauritzen, G., Olesen, C. W., Hansen, S. H., Bødtkjer, E., Pedersen, Stine Helene Falsig & Bunch, Lennart, 2012, In: ChemMedChem. 7, 10, p. 1808-1814 7 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Heterocycles as nonclassical bioisosteres of alpha-amino acids
Poulie, Christian Bernard Matthijs & Bunch, Lennart, Feb 2013, In: ChemMedChem. 8, 2, p. 205-215Research output: Contribution to journal › Journal article › Research › peer-review
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Ibotenic acid and thioibotenic acid: a remarkable difference in activity at group III metabotropic glutamate receptors
Hermit, M. B., Greenwood, J. R., Nielsen, Birgitte, Bunch, Lennart, Jørgensen, Charlotte Grube, Vestergaard, H. T., Stensbøl, T. B., Sanchez, C., Krogsgaard-Larsen, Povl, Madsen, Ulf & Bräuner, Hans, 23 Feb 2004, In: European Journal of Pharmacology. 486, 3, p. 241-50Research output: Contribution to journal › Journal article › Research › peer-review
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Identification and Structure-Activity Relationship Study of Imidazo[1,2-a]pyridine-3-amines as First Selective Inhibitors of Excitatory Amino Acid Transporter Subtype 3 (EAAT3)
Wu, P., Bjørn-Yoshimoto, Walden, Staudt, Markus, Jensen, Anders A. & Bunch, Lennart, 2019, In: ACS Chemical Neuroscience. 10, p. 4414-4429Research output: Contribution to journal › Journal article › Research › peer-review
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Identification of a New Class of Selective Excitatory Amino Acid Transporter Subtype 1 (EAAT1) Inhibitors Followed by a Structure-Activity-Relationship Study
Hansen, S. W., Erichsen, M. N., Fu, B., Bjørn-Yoshimoto, Walden, Abrahamsen, B., Hansen, J. C., Jensen, Anders A. & Bunch, Lennart, 2016, In: Journal of Medicinal Chemistry. 59, 19, p. 8757-8770 14 p.Research output: Contribution to journal › Journal article › Research › peer-review
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In vitro ADME characterization of a very potent 3-acylamino-2-aminopropionic acid-derived GluN2C-NMDA receptor agonist and its ester prodrugs
Bechthold, E., Grey, L., Diamant, E., Schmidt, J., Steigerwald, R., Zhao, F., Hansen, K. B., Bunch, Lennart, Clausen, Rasmus Prætorius & Wünsch, B., 2023, In: Biological Chemistry. 404, 4, p. 255-265Research output: Contribution to journal › Journal article › Research › peer-review
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Introduction to drug design and discovery
Krogsgaard-Larsen, Povl & Bunch, Lennart, 2010, Textbook of drug design and discovery. Krogsgaard-Larsen, P., Strømgaard, K. & Madsen, U. (eds.). 4 ed. Boca Raton: CRC Press, p. 1-13Research output: Chapter in Book/Report/Conference proceeding › Book chapter › Education
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Medicinal chemistry of competitive kainate receptor antagonists
Larsen, A. M. & Bunch, Lennart, 16 Feb 2011, In: ACS Chemical Neuroscience. 2, 2, p. 60-74Research output: Contribution to journal › Review › Research › peer-review
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Mixed cyano-gilman cuprates - Advances in conjugate addition to alpha,beta-unsaturated pyroglutaminol
Bunch, Lennart, Krogsgaard-Larsen, Povl & Madsen, Ulf, Jan 2002, In: Synthesis. 1, p. 31-33Research output: Contribution to journal › Journal article › Research › peer-review
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Molecular recognition of two 2,4-syn-functionalized (S)-glutamate analogues by the kainate receptor GluK3 ligand-binding domain
Venskutonyte, R., Larsen, A. P., Frydenvang, Karla Andrea, Gajhede, Michael, Gefflaut, T., Pickering, Darryl S, Bunch, Lennart & Kastrup, Jette Sandholm Jensen, 2014, In: ChemMedChem. 9, 10, p. 2254-2259 6 p.Research output: Contribution to journal › Journal article › Research › peer-review
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New 4-Functionalized Glutamate Analogues Are Selective Agonists at Metabotropic Glutamate Receptor Subtype 2 or Selective Agonists at Metabotropic Glutamate Receptor Group III
Huynh, Tri Hien Viet, Erichsen, M. N., Tora, A. S., Goudet, C., Sagot, E., Assaf, Z., Thomsen, C., Brodbeck, R., Stensbol, T. B., Bjørn-Yoshimoto, Walden, Nielsen, Birgitte, Pin, J., Gefflaut, T. & Bunch, Lennart, 2016, In: Journal of Medicinal Chemistry. 59, 3, p. 914-924 11 p.Research output: Contribution to journal › Journal article › Research › peer-review
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New Palladium-Catalyzed Domino Reaction with Intramolecular Ring Closure of an N-(2-Chloro-3-heteroaryl) arylamide: First Synthesis of Oxazolo[4,5-b] pyrazines
Demmer, C. S., Hansen, J. C., Kehler, J. & Bunch, Lennart, 24 Mar 2014, In: Advanced Synthesis & Catalysis. 356, 5, p. 1047-1055 9 p.Research output: Contribution to journal › Journal article › Research › peer-review
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New insights into the structure-activity-relationship of selective excitatory amino acid transporter subtype 1 (EAAT1) inhibitors UCPH-101 and UCPH-102
Hansen, S. W., Erichsen, M. N., Huynh, Tri Hien Viet, Ruiz, J. A., Haym, I., Bjørn-Yoshimoto, Walden, Abrahamsen, B., Hansen, Jeanette Venla, Storgaard, M., Eriksen, A. L., Jensen, Anders A. & Bunch, Lennart, 2016, In: ChemMedChem. 11, 4, p. 382-402 21 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Pharmacological and structural characterization of conformationally restricted (S)-glutamate analogues at ionotropic glutamate receptors
Juknaite, L., Venskutonyte, R., Assaf, Z., Faure, S., Gefflaut, T., Aitken, D. J., Nielsen, Birgitte, Gajhede, Michael, Kastrup, Jette Sandholm Jensen, Bunch, Lennart, Frydenvang, Karla Andrea & Pickering, Darryl S, 2012, In: Journal of Structural Biology. 180, 1, p. 39-46Research output: Contribution to journal › Journal article › Research › peer-review
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Pharmacological characterization of (4R)-alkyl glutamate analogues at the ionotropic glutamate receptors: focus on subtypes iGlu5-7
Bunch, Lennart, Gefflaut, T., Alaux, S., Sagot, E., Nielsen, Birgitte & Pickering, Darryl S, 2009, In: European Journal of Pharmacology. 609, p. 1-4Research output: Contribution to journal › Journal article › Research › peer-review
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Physiology, pharmacology and pathophysiology of the pH regulatory transport proteins NHE1 and NBCn1: similarities, differences, and implications for cancer therapy
Bødtkjer, E., Bunch, Lennart & Pedersen, Stine Helene Falsig, 2012, In: Current Pharmaceutical Design. 18, 10, p. 1345-1371 27 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Probing for improved potency and in vivo bioavailability of excitatory amino acid transporter subtype 1 inhibitors UCPH-101 and UCPH-102: Design, synthesis and pharmacological evaluation of substituted 7-biphenyl analogs
Erichsen, M. N., Hansen, J., Artacho Ruiz, J., Demmer, C. S., Abrahamsen, B., Bastlund, J. F., Bundgaard, C., Jensen, Anders A. & Bunch, Lennart, 2014, In: Neurochemical Research. 39, 10, p. 1964-1979 16 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Profiling substrate specificity of two series of phenethylamine analogs at monoamine oxidase A and B
Heuson, E., Storgaard, M., Huynh, Tri Hien Viet, Charmantray, F., Gefflaut, T. & Bunch, Lennart, 2014, In: Organic & Biomolecular Chemistry. 12, 43, p. 8689-8695 7 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Rational Design, Synthesis and Pharmacological Evaluation of the (2R)- and (2S)-Stereoisomers of 3-(2-Carboxypyrrolidinyl)-2-methyl Acetic Acid as Ligands for the Ionotropic Glutamate Receptors.
Rasmussen, J., Storgaard, M., Pickering, Darryl S & Bunch, Lennart, 7 Mar 2011, In: ChemMedChem. 6, 3, p. 498-504 7 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Rational design and enantioselective synthesis of (1R,4S,5R,6S)-3-azabicyclo[3.3.0]octane-4,6-dicarboxylic acid - a novel inhibitor at human glutamate transporter subtypes 1, 2, and 3
Bunch, Lennart, Nielsen, Birgitte, Jensen, Anders A. & Bräuner, Hans, 2006, In: Journal of Medicinal Chemistry. 49, 1, p. 172-8 7 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Rational design, synthesis, and pharmacological evaluation of 2-azanorbornane-3-exo,5-endo-dicarboxylic acid: a novel conformationally restricted glutamic acid analogue
Bunch, Lennart, Liljefors, T., Greenwood, J. R., Frydenvang, Karla Andrea, Bräuner, Hans, Krogsgaard-Larsen, Povl & Madsen, Ulf, 2003, In: Journal of Organic Chemistry. 68, 4, p. 1489-95 7 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Regioselective lithiation and functionalization of 3-(benzyloxy)isothiazole: Application to the synthesis of thioibotenic acid
Bunch, Lennart, Krogsgaard-Larsen, Povl & Madsen, Ulf, 5 Apr 2002, In: Journal of Organic Chemistry. 67, 7, p. 2375-2377Research output: Contribution to journal › Journal article › Research › peer-review
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Review on modern advances of chemical methods for the introduction of a phosphonic acid group
Demmer, C. S., Krogsgaard-Larsen, N. & Bunch, Lennart, 2011, In: Chemical Reviews. 111, 12, p. 7981-8006Research output: Contribution to journal › Review › Research › peer-review
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Revisiting the Quinoxalinedione scaffold in the Construction of New Ligands for the Ionotropic Glutamate Receptors.
Demmer, C. S., Rombach, D., Liu, N., Nielsen, Birgitte, Pickering, Darryl S & Bunch, Lennart, 1 Dec 2017, In: A C S Chemical Neuroscience. 8, 11, p. 2477-2495 19 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Semi-synthesis of novel buprenorphine derivatives and their anti-nociceptive properties and dependency potential
Hasanpour, Z., Salehi, P., Bunch, Lennart, Khoramjouy, M., Bararjanian, M., Stærk, Dan & Faizi, M., 2021, In: Canadian Journal of Chemistry. 99, 11, p. 910-919Research output: Contribution to journal › Journal article › Research › peer-review
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Stereocontrolled synthesis and pharmacological evaluation of azetidine-2,3-dicarboxylic acids at NMDA receptors
Sivaprakasam, M., Hansen, K. B., David, O., Nielsen, Birgitte, Traynelis, S. F., Clausen, Rasmus Prætorius, Couty, F. & Bunch, Lennart, 2009, In: ChemMedChem. 4, 1, p. 110-117Research output: Contribution to journal › Journal article › Research › peer-review
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Stereoselective Synthesis of New (2S,3R)-3-Carboxyphenyl)pyrrolidine-2-carboxylic Acid Analogues Utilizing a C(sp3)-H Activation Strategy and Structure-Activity Relationship Studies at the Ionotropic Glutamate Receptors
Kayser, S., Hansen, J. C., Staudt, Markus, Moroz, A., Larsen, Y., Temperini, Piero, Yi, F., Syrenne, J. T., Krogsgaard-Larsen, N., Iliadis, S., Nielsen, Birgitte, Hansen, K. B., Pickering, Darryl S & Bunch, Lennart, 2020, In: ACS Chemical Neuroscience. 11, p. 674-701 28 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Stereoselective chemoenzymatic synthesis of the four stereoisomers of l-2-(2-carboxycyclobutyl)glycine and pharmacological characterization at human excitatory amino acid transporter subtypes 1, 2, and 3
Faure, S., Jensen, Anders A., Maurat, V., Gu, X., Sagot, E., Aitken, D. J., Bolte, J., Gefflaut, T. & Bunch, Lennart, 2006, In: Journal of Medicinal Chemistry. 49, 22, p. 6532-8 7 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Structure-Activity Relationship Study of Ionotropic Glutamate Receptor Antagonist (2S,3R)-3-(3-Carboxyphenyl)pyrrolidine-2-carboxylic Acid
Krogsgaard-Larsen, N., Storgaard, M., Møller, C., Demmer, C. S., Hansen, J., Han, L., Monrad, R. N., Nielsen, Birgitte, Tapken, D., Pickering, Darryl S, Kastrup, Jette Sandholm Jensen, Frydenvang, Karla Andrea & Bunch, Lennart, 2015, In: Journal of Medicinal Chemistry. 58, 15, p. 6131-50 20 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Structure-activity relationship study of first selective inhibitor of excitatory amino acid transporter subtype 1: 2-amino-4-(4-methoxyphenyl)-7-(naphthalen-1-yl)-5-oxo-5,6,7,8-tetrahydro-4H-chromene-3-carbonitrile (UCPH-101)
Erichsen, M. N., Huynh, Tri Hien Viet, Abrahamsen, B., Bastlund, J. F., Bundgaard, C., Monrad, O., Bekker-Jensen, A., Nielsen, C. W., Frydenvang, Karla Andrea, Jensen, Anders A. & Bunch, Lennart, 2010, In: Journal of Medicinal Chemistry. 53, 19, p. 7180–7191Research output: Contribution to journal › Journal article › Research › peer-review
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Structure-activity relationship study of selective excitatory amino acid transporter subtype 1 (EAAT1) inhibitor 2-amino-4-(4-methoxyphenyl)-7-(naphthalen-1-yl)-5-oxo-5,6,7,8-tetrahydro-4H-chromene-3-carbonitrile (UCPH-101) and absolute configurational assignment using infrared and vibrational circular dichroism spectroscopy in combination with ab initio hartree-fock calculations
Huynh, Tri Hien Viet, Shim, I., Bohr, H., Abrahamsen, B., Nielsen, Birgitte, Jensen, Anders A. & Bunch, Lennart, 2012, In: Journal of Medicinal Chemistry. 55, 11, p. 5403-12 10 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Structure-activity-relationship study of N-acyl-N-phenylpiperazines as potential inhibitors of the excitatory amino acid transporters (EAATs): Improving the potency of a micromolar screening hit is not truism
Huynh, Tri Hien Viet, Demmer, C. S., Abrahamsen, B., Marcher, Emil, Frykman, M., Jensen, Anders A. & Bunch, Lennart, 2013, In: SpringerPlus. 2, p. 112Research output: Contribution to journal › Journal article › Research › peer-review
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Study of Oxidative Cyclization Using PhI(OAc)(2) in the Formation of Benzo[4,5]thiazolo[2,3-c][1,2,4]triazoles and Related Heterocycles - Scope and Limitations
Demmer, C. S., Jorgensen, M., Kehler, J. & Bunch, Lennart, Jun 2014, In: SYNLETT: Accounts and Rapid Communications in Chemical Synthesis. 25, 9, p. 1279-1282 4 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Subtype selective kainic acid receptor agonists: discovery and approaches to rational design
Bunch, Lennart & Krogsgaard-Larsen, Povl, 2009, In: Medicinal Research Reviews. 29, 1, p. 3-28Research output: Contribution to journal › Review › Research › peer-review
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Synthesis and Pharmacological Characterization of the Selective GluK1 Radioligand (S)-2-Amino-3-(6-[3H]-2,4-dioxo-3,4-dihydrothieno[3,2-d]pyrimidin-1(2H)-yl)propanoic acid ([3H]-NF608)
Alcaide, A., Marconi, L., Marek, A., Haym, I., Nielsen, Birgitte, Møllerud, S., Jensen, M., Conti, P., Pickering, Darryl S & Bunch, Lennart, 2016, In: MedChemComm. 7, p. 2136-2144 9 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Synthesis and Selective Functionalization of [1,2,4]Triazolo[4,3-a]pyrazines
Demmer, C. S., Jorgensen, M., Kehler, J., Bunch, Lennart & Rasmussen, L. K., 2015, In: SYNLETT: Accounts and Rapid Communications in Chemical Synthesis. 26, 4, p. 519-524 6 p.Research output: Contribution to journal › Letter › Research › peer-review
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Synthesis and pharmacological characterization of conformationally restricted 2-amino-Adipic acid analogs and carboxycyclopropyl glycines as selective metabotropic glutamate 2 receptor agonists
Staudt, Markus, Liu, N., Malhaire, F., Doroudian, Yasaman, Prézeau, L., Renard, E., Hasanpour, Z., Pin, J. P. & Bunch, Lennart, 2024, In: European Journal of Medicinal Chemistry. 266, 11 p., 116157.Research output: Contribution to journal › Journal article › Research › peer-review
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Synthesis and receptor binding affinity of new selective GluR5 ligands
Bunch, Lennart, Johansen, T. H., Bräuner, Hans, Stensbøl, T. B., Johansen, Tommy Nørskov, Krogsgaard-Larsen, Povl & Madsen, Ulf, Apr 2001, In: Bioorganic & Medicinal Chemistry. 9, 4, p. 875-9Research output: Contribution to journal › Journal article › Research › peer-review
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Synthesis of (3-hydroxy-pyrazolin-5-yl)glycine based ligands interacting with ionotropic glutamate receptors
Pinto, A., Tamborini, L., Mastronardi, F., Ettari, R., Safoz, Y., Bunch, Lennart, Nielsen, Birgitte, Jensen, Anders A., De Micheli, C. & Conti, P., 2014, In: European Journal of Medicinal Chemistry. 75, p. 151-158 8 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Synthesis of Polysubstituted Meta-Halophenols by Anion-Accelerated 2π-Electrocyclic Ring-Opening
Staudt, Markus, Sølling, Theis Ivan & Bunch, Lennart, 2021, In: Chemistry - A European Journal. 27, 42, p. 10941–10947 7 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Synthesis of phenol derivatives from cyclopentenones with arynes as key intermediates
Telese, D., Staudt, Markus & Bunch, Lennart, 2022, In: Results in Chemistry. 4, 7 p., 100412.Research output: Contribution to journal › Journal article › Research › peer-review
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Tetrabutylammonium Fluoride (TBAF) as a Mild and Versatile Reagent for Cleaving Boroxazolidones to their Corresponding Free α-Amino Acids
Poulie, Christian Bernard Matthijs & Bunch, Lennart, Mar 2017, In: European Journal of Organic Chemistry. 11, p. 1475-1478Research output: Contribution to journal › Journal article › Research › peer-review
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The Screening and Design of Allosteric Kinase Inhibitors
Wu, P., Dinér, P. & Bunch, Lennart, 2019, Kinase Drug Discovery: Modern Approaches. 1. ed. Royal Society of Chemistry, p. 34-60Research output: Chapter in Book/Report/Conference proceeding › Book chapter › Research › peer-review
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The glutamate transport inhibitor DL-Threo-β-Benzyloxyaspartic acid (DL-TBOA) differentially affects SN38- and oxaliplatin-induced death of drug-resistant colorectal cancer cells
Cuesta, E. P., Christensen, S., Jensen, Anders A., Jensen, N. F., Bunch, Lennart, Rømer, M. U. K., Brünner, N., Stenvang, Jan & Pedersen, Stine Helene Falsig, 2015, In: B M C Cancer. 15, 1, 17 p., 411.Research output: Contribution to journal › Journal article › Research › peer-review
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Transition Metal-Free Synthesis of meta-Bromo- and meta-Trifluoromethylanilines from Cyclopentanones by a Cascade Reaction
Staudt, Markus, Cetin, A. & Bunch, Lennart, 2022, In: Chemistry: A European Journal. 28, 10, 5 p., 202102998.Research output: Contribution to journal › Journal article › Research › peer-review
- Published
Unprecedented migration of N-alkoxycarbonyl groups in protected pyroglutaminol
Bunch, Lennart, Norrby, P., Frydenvang, Karla Andrea, Krogsgaard-Larsen, Povl & Madsen, Ulf, 2001, In: Organic Letters. 3, 3, p. 433-5 3 p.Research output: Contribution to journal › Journal article › Research › peer-review
- Published
β-Indolyloxy Functionalized Aspartate Analogs as Inhibitors of the Excitatory Amino Acid Transporters (EAATs)
Liu, N., Jensen, Anders A. & Bunch, Lennart, 2020, In: ACS Medicinal Chemistry Letters. 11, 11, p. 2212-2220 9 p.Research output: Contribution to journal › Journal article › Research › peer-review
ID: 1302517
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The glutamate transport inhibitor DL-Threo-β-Benzyloxyaspartic acid (DL-TBOA) differentially affects SN38- and oxaliplatin-induced death of drug-resistant colorectal cancer cells
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Chemoenzymatic synthesis and pharmacological characterization of functionalized aspartate analogues as novel excitatory amino acid transporter inhibitors
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Synthesis of phenol derivatives from cyclopentenones with arynes as key intermediates
Research output: Contribution to journal › Journal article › Research › peer-review
Published