Lennart Bunch

Lennart Bunch

Professor

ORCID: 0000-0002-0180-4639

Publication year:
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1 - 85 out of 85Page size: 500
  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 journal › Journal article › Research › peer-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 journal › Journal article › Research › peer-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 journal › Journal article › Research › peer-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 journal › Journal article › Research › peer-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 journal › Journal article › Research › peer-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 journal › Journal article › Research › peer-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 journal › Journal article › Research › peer-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 journal › Journal article › Research › peer-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 journal › Journal article › Research › peer-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 journal › Journal article › Research › peer-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 journal › Journal article › Research › peer-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 journal › Journal article › Research › peer-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 journal › Journal article › Research › peer-review

  19. Published

    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. 4362-4375

    Research output: Contribution to journal › Journal article › Research › peer-review

  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 journal › Journal article › Research › peer-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 journal › Journal article › Research › peer-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 journal › Journal article › Research › peer-review

  24. Published

    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. 4414-4429

    Research output: Contribution to journal › Journal article › Research › peer-review

  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 proceeding › Book chapter › Research › peer-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 journal › Journal article › Research › peer-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 journal › Journal article › Research › peer-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 journal › Journal article › Research › peer-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 journal › Journal article › Research › peer-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 journal › Journal article › Research › peer-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 journal › Journal article › Research › peer-review

  34. Published

    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

  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 journal › Journal article › Research › peer-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 journal › Journal article › Research › peer-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 journal › Journal article › Research › peer-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 journal › Journal article › Research › peer-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 journal › Journal article › Research › peer-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 journal › Journal article › Research › peer-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 journal › Journal article › Research › peer-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 journal › Journal article › Research › peer-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 journal › Journal article › Research › peer-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 journal › Journal article › Research › peer-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 journal › Journal article › Research › peer-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 journal › Journal article › Research › peer-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 journal › Letter › Research › peer-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 journal › Journal article › Research › peer-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 journal › Journal article › Research › peer-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 journal › Journal article › Research › peer-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 journal › Journal article › Research › peer-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 journal › Journal article › Research › peer-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 journal › Journal article › Research › peer-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 journal › Journal article › Research › peer-review

  58. 2013
  59. 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

  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 journal › Comment/debate › Research › peer-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 journal › Journal article › Research › peer-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 journal › Journal article › Research › peer-review

  63. 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. 1614-1628

    Research output: Contribution to journal › Journal article › Research › peer-review

  64. 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. 112

    Research output: Contribution to journal › Journal article › Research › peer-review

  65. 2012
  66. 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. 6831-6839

    Research output: Contribution to journal › Journal article › Research › peer-review

  67. 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

  68. 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. 39-46

    Research output: Contribution to journal › Journal article › Research › peer-review

  69. 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

  70. 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

  71. 2011
  72. 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. 307-314

    Research output: Contribution to journal › Journal article › Research › peer-review

  73. 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

  74. 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. 887-906

    Research output: Contribution to journal › Review › Research › peer-review

  75. 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

  76. Published

    Medicinal chemistry of competitive kainate receptor antagonists

    Larsen, A. M. & Bunch, Lennart, 16 Feb 2011, In: ACS Chemical Neuroscience. 2, 2, p. 60-74

    Research output: Contribution to journal › Review › Research › peer-review

  77. 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. 7981-8006

    Research output: Contribution to journal › Review › Research › peer-review

  78. 2010
  79. 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. 1-13

    Research output: Chapter in Book/Report/Conference proceeding › Book chapter › Education

  80. Published

    Selective inhibitors of the excitatory amino acid transporter subtype 1 (EAAT1/GLAST)

    Bunch, Lennart & Jensen, Anders A., 2010, Patent No. WO/2010/066253

    Research output: Patent

  81. 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. 7180–7191

    Research output: Contribution to journal › Journal article › Research › peer-review

  82. 2009
  83. 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. 1925-1929

    Research output: Contribution to journal › Journal article › Research › peer-review

  84. 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. 912-915

    Research output: Contribution to journal › Journal article › Research › peer-review

  85. 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. 719-731

    Research output: Contribution to journal › Journal article › Research › peer-review

  86. 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. 1-4

    Research output: Contribution to journal › Journal article › Research › peer-review

  87. 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. 110-117

    Research output: Contribution to journal › Journal article › Research › peer-review

  88. 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. 3-28

    Research output: Contribution to journal › Review › Research › peer-review

  89. 2008
  90. 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

  91. 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. 4093-103

    Research output: Contribution to journal › Journal article › Research › peer-review

  92. 2006
  93. 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. 2148-2154

    Research output: Contribution to journal › Journal article › Research › peer-review

  94. 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

  95. 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

  96. 2005
  97. 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

  98. 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

  99. 2004
  100. 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. 241-50

    Research output: Contribution to journal › Journal article › Research › peer-review

  101. 2003
  102. 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

  103. 2002
  104. 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. 2375-2377

    Research output: Contribution to journal › Journal article › Research › peer-review

  105. 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. 31-33

    Research output: Contribution to journal › Journal article › Research › peer-review

  106. 2001
  107. 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. 875-9

    Research output: Contribution to journal › Journal article › Research › peer-review

  108. 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

ID: 1302517