Lennart Bunch
Professor
Medicinal Chemistry
Jagtvej 162
2100 København Ø
- 2001
- 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
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
- 2002
- Published
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
- Published
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
- 2003
- Published
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
- 2004
- Published
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
- 2005
- Published
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
- Published
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
- 2006
- Published
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
- Published
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
- Published
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
- 2008
- Published
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
- Published
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
- 2009
- Published
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
- Published
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
- Published
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
- Published
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
- Published
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
- Published
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
- 2010
- Published
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
- Published
- Published
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
- 2011
- Published
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
- Published
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
- Published
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
- Published
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
- Published
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
- Published
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
- 2012
- Published
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
- Published
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
- Published
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
- Published
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
- Published
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
- 2013
- Published
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
- Published
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
- Published
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
- Published
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
- Published
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
- Published
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
- 2014
- Published
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
- Published
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
- Published
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
- Published
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
- Published
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
- Published
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
- 2015
- Published
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
- Published
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
- Published
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
- Published
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
- Published
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
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
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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
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