Lennart Bunch

Lennart Bunch

Professor


  1. 2024
  2. Published

    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. 1314–1326

    Research output: Contribution to journalJournal articleResearchpeer-review

  3. Published

    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 journalJournal articleResearchpeer-review

  4. 2023
  5. Published

    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. 326-333

    Research output: Contribution to journalJournal articleResearchpeer-review

  6. Published

    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. 255-265

    Research output: Contribution to journalJournal articleResearchpeer-review

  7. 2022
  8. Published

    (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. 1580–1587

    Research output: Contribution to journalJournal articleResearchpeer-review

  9. Published

    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. 734-746

    Research output: Contribution to journalJournal articleResearchpeer-review

  10. Published

    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 journalJournal articleResearchpeer-review

  11. Published

    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 journalJournal articleResearchpeer-review

  12. Published

    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 journalJournal articleResearchpeer-review

  13. 2021
  14. Published

    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. 910-919

    Research output: Contribution to journalJournal articleResearchpeer-review

  15. Published

    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 journalJournal articleResearchpeer-review

  16. 2020
  17. Published

    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 journalJournal articleResearchpeer-review

  18. Published

    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 journalJournal articleResearchpeer-review

  19. Published
  20. Published

    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 journalJournal articleResearchpeer-review

  21. 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 journalJournal articleResearchpeer-review

  22. 2019
  23. Published

    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 journalJournal articleResearchpeer-review

  24. Published
  25. Published

    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. 34-60

    Research output: Chapter in Book/Report/Conference proceedingBook chapterResearchpeer-review

  26. 2018
  27. Published

    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. 7741-7753

    Research output: Contribution to journalJournal articleResearchpeer-review

  28. Published

    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. 3904-3913

    Research output: Contribution to journalJournal articleResearchpeer-review

  29. Published

    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. 305-319

    Research output: Contribution to journalJournal articleResearchpeer-review

  30. 2017
  31. Published

    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 journalJournal articleResearchpeer-review

  32. Published

    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 journalJournal articleResearchpeer-review

  33. Published

    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. 1475-1478

    Research output: Contribution to journalJournal articleResearchpeer-review

  34. Published
  35. 2016
  36. Published

    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 journalJournal articleResearchpeer-review

  37. Published

    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 journalJournal articleResearchpeer-review

  38. Published

    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 journalJournal articleResearchpeer-review

  39. Published

    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 journalJournal articleResearchpeer-review

  40. Published

    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 journalJournal articleResearchpeer-review

  41. Published

    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 journalJournal articleResearchpeer-review

  42. 2015
  43. Published

    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 journalJournal articleResearchpeer-review

  44. Published

    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 journalJournal articleResearchpeer-review

  45. 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 journalJournal articleResearchpeer-review

  46. 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 journalJournal articleResearchpeer-review

  47. 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 journalJournal articleResearchpeer-review

  48. 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 journalJournal articleResearchpeer-review

  49. 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 journalLetterResearchpeer-review

  50. Published

    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 journalJournal articleResearchpeer-review

  51. 2014
  52. 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 journalJournal articleResearchpeer-review

  53. 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 journalJournal articleResearchpeer-review

  54. 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 journalJournal articleResearchpeer-review

  55. 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 journalJournal articleResearchpeer-review

  56. 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 journalJournal articleResearchpeer-review

  57. 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 journalJournal articleResearchpeer-review

  58. 2013
  59. Published
  60. 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 journalComment/debateResearchpeer-review

  61. Published

    Heterocycles as nonclassical bioisosteres of alpha-amino acids

    Poulie, Christian Bernard Matthijs & Bunch, Lennart, Feb 2013, In: ChemMedChem. 8, 2, p. 205-215

    Research output: Contribution to journalJournal articleResearchpeer-review

  62. 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. 1068-1087

    Research output: Contribution to journalJournal articleResearchpeer-review

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