Lennart Bunch
Professor
Medicinal Chemistry
Jagtvej 162
2100 København Ø
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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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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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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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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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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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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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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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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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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
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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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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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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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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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(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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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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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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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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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 (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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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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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
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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 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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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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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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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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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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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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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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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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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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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
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
Research 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
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
Research output: Contribution to journal › Journal article › Research › peer-review
Published