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Page 1
GluK1 antagonists from 6-(carboxy)phenyl decahydroisoquinoline derivatives. SAR and evaluation of a prodrug strategy for oral efficacy in pain models.
Martinez-Perez JA, Iyengar S, Shannon HE, Bleakman D, Alt A, Arnold BM, Bell MG, Bleisch TJ, Castaño AM, Del Prado M, Dominguez E, Escribano AM, Filla SA, Ho KH, Hudziak KJ, Jones CK, Mateo A, Mathes BM, Mattiuz EL, Ogden AM, Simmons RM, Stack DR, Stratford RE, Winter MA, Wu Z, Ornstein PL. Martinez-Perez JA, et al. Among authors: mathes bm. Bioorg Med Chem Lett. 2013 Dec 1;23(23):6459-62. doi: 10.1016/j.bmcl.2013.09.046. Epub 2013 Sep 25. Bioorg Med Chem Lett. 2013. PMID: 24119554
Ethyl (3S,4aR,6S,8aR)-6-(4-ethoxycar- bonylimidazol-1-ylmethyl)decahydroiso-quinoline-3-carboxylic ester: a prodrug of a GluR5 kainate receptor antagonist active in two animal models of acute migraine.
Filla SA, Winter MA, Johnson KW, Bleakman D, Bell MG, Bleisch TJ, Castaño AM, Clemens-Smith A, del Prado M, Dieckman DK, Dominguez E, Escribano A, Ho KH, Hudziak KJ, Katofiasc MA, Martinez-Perez JA, Mateo A, Mathes BM, Mattiuz EL, Ogden AM, Phebus LA, Stack DR, Stratford RE, Ornstein PL. Filla SA, et al. Among authors: mathes bm. J Med Chem. 2002 Sep 26;45(20):4383-6. doi: 10.1021/jm025548q. J Med Chem. 2002. PMID: 12238915
Two prodrugs of potent and selective GluR5 kainate receptor antagonists actives in three animal models of pain.
Dominguez E, Iyengar S, Shannon HE, Bleakman D, Alt A, Arnold BM, Bell MG, Bleisch TJ, Buckmaster JL, Castano AM, Del Prado M, Escribano A, Filla SA, Ho KH, Hudziak KJ, Jones CK, Martinez-Perez JA, Mateo A, Mathes BM, Mattiuz EL, Ogden AM, Simmons RM, Stack DR, Stratford RE, Winter MA, Wu Z, Ornstein PL. Dominguez E, et al. Among authors: mathes bm. J Med Chem. 2005 Jun 30;48(13):4200-3. doi: 10.1021/jm0491952. J Med Chem. 2005. PMID: 15974569
GluK1 antagonists from 6-(tetrazolyl)phenyl decahydroisoquinoline derivatives: in vitro profile and in vivo analgesic efficacy.
Martinez-Perez JA, Iyengar S, Shannon HE, Bleakman D, Alt A, Clawson DK, Arnold BM, Bell MG, Bleisch TJ, Castaño AM, Del Prado M, Dominguez E, Escribano AM, Filla SA, Ho KH, Hudziak KJ, Jones CK, Mateo A, Mathes BM, Mattiuz EL, Ogden AM, Simmons RM, Stack DR, Stratford RE, Winter MA, Wu Z, Ornstein PL. Martinez-Perez JA, et al. Among authors: mathes bm. Bioorg Med Chem Lett. 2013 Dec 1;23(23):6463-6. doi: 10.1016/j.bmcl.2013.09.045. Epub 2013 Sep 24. Bioorg Med Chem Lett. 2013. PMID: 24140446
Discovery of selective N-[3-(1-methyl-piperidine-4-carbonyl)-phenyl]-benzamide-based 5-HT₁ F receptor agonists: Evolution from bicyclic to monocyclic cores.
Zhang D, Blanco MJ, Ying BP, Kohlman D, Liang SX, Victor F, Chen Q, Krushinski J, Filla SA, Hudziak KJ, Mathes BM, Cohen MP, Zacherl D, Nelson DL, Wainscott DB, Nutter SE, Gough WH, Schaus JM, Xu YC. Zhang D, et al. Among authors: mathes bm. Bioorg Med Chem Lett. 2015 Oct 1;25(19):4337-41. doi: 10.1016/j.bmcl.2015.07.042. Epub 2015 Jul 22. Bioorg Med Chem Lett. 2015. PMID: 26271587
Preparation and biological evaluation of conformationally constrained BACE1 inhibitors.
Winneroski LL, Schiffler MA, Erickson JA, May PC, Monk SA, Timm DE, Audia JE, Beck JP, Boggs LN, Borders AR, Boyer RD, Brier RA, Hudziak KJ, Klimkowski VJ, Garcia Losada P, Mathes BM, Stout SL, Watson BM, Mergott DJ. Winneroski LL, et al. Among authors: mathes bm. Bioorg Med Chem. 2015 Jul 1;23(13):3260-8. doi: 10.1016/j.bmc.2015.04.062. Epub 2015 May 6. Bioorg Med Chem. 2015. PMID: 26001341
Preparation and biological evaluation of BACE1 inhibitors: Leveraging trans-cyclopropyl moieties as ligand efficient conformational constraints.
Winneroski LL, Erickson JA, Green SJ, Lopez JE, Stout SL, Porter WJ, Timm DE, Audia JE, Barberis M, Beck JP, Boggs LN, Borders AR, Boyer RD, Brier RA, Hembre EJ, Hendle J, Garcia-Losada P, Minguez JM, Mathes BM, May PC, Monk SA, Rankovic Z, Shi Y, Watson BM, Yang Z, Mergott DJ. Winneroski LL, et al. Among authors: mathes bm. Bioorg Med Chem. 2020 Jan 1;28(1):115194. doi: 10.1016/j.bmc.2019.115194. Epub 2019 Nov 15. Bioorg Med Chem. 2020. PMID: 31786008
Synthesis and Preclinical Characterization of LY3154885, a Human Dopamine D1 Receptor Positive Allosteric Modulator with an Improved Nonclinical Drug-Drug Interaction Risk Profile.
Hao J, Beck J, Zhou X, Lackner GL, Johnston R, Reinhard M, Goldsmith P, Hollinshead S, Dehlinger V, Filla SA, Wang XS, Richardson J, Posada M, Mohutsky M, Schober D, Katner JS, Chen Q, Hu B, Remick DM, Coates DA, Mathes BM, Hawk MK, Svensson KA, Hembre E. Hao J, et al. Among authors: mathes bm. J Med Chem. 2022 Mar 10;65(5):3786-3797. doi: 10.1021/acs.jmedchem.1c01887. Epub 2022 Feb 17. J Med Chem. 2022. PMID: 35175768
49 results