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Page 1
CoMFA, synthesis, and pharmacological evaluation of (E)-3-(2-carboxy-2-arylvinyl)-4,6-dichloro-1H-indole-2-carboxylic acids: 3-[2-(3-aminophenyl)-2-carboxyvinyl]-4,6-dichloro-1H-indole-2-carboxylic acid, a potent selective glycine-site NMDA receptor antagonist.
Baron BM, Cregge RJ, Farr RA, Friedrich D, Gross RS, Harrison BL, Janowick DA, Matthews D, McCloskey TC, Meikrantz S, Nyce PL, Vaz R, Metz WA. Baron BM, et al. Among authors: gross rs. J Med Chem. 2005 Feb 24;48(4):995-1018. doi: 10.1021/jm0491849. J Med Chem. 2005. PMID: 15715469
Design and synthesis of tricyclic corticotropin-releasing factor-1 antagonists.
Gross RS, Guo Z, Dyck B, Coon T, Huang CQ, Lowe RF, Marinkovic D, Moorjani M, Nelson J, Zamani-Kord S, Grigoriadis DE, Hoare SR, Crowe PD, Bu JH, Haddach M, McCarthy J, Saunders J, Sullivan R, Chen T, Williams JP. Gross RS, et al. J Med Chem. 2005 Sep 8;48(18):5780-93. doi: 10.1021/jm049085v. J Med Chem. 2005. PMID: 16134945
2-Amino-N-pyrimidin-4-ylacetamides as A2A receptor antagonists: 1. Structure-activity relationships and optimization of heterocyclic substituents.
Slee DH, Chen Y, Zhang X, Moorjani M, Lanier MC, Lin E, Rueter JK, Williams JP, Lechner SM, Markison S, Malany S, Santos M, Gross RS, Jalali K, Sai Y, Zuo Z, Yang C, Castro-Palomino JC, Crespo MI, Prat M, Gual S, Díaz JL, Saunders J. Slee DH, et al. Among authors: gross rs. J Med Chem. 2008 Mar 27;51(6):1719-29. doi: 10.1021/jm701185v. Epub 2008 Feb 29. J Med Chem. 2008. PMID: 18307292
When structure-affinity relationships meet structure-kinetics relationships: 3-((Inden-1-yl)amino)-1-isopropyl-cyclopentane-1-carboxamides as CCR2 antagonists.
Vilums M, Zweemer AJ, Barmare F, van der Gracht AM, Bleeker DC, Yu Z, de Vries H, Gross R, Clemens J, Krenitsky P, Brussee J, Stamos D, Saunders J, Heitman LH, IJzerman AP. Vilums M, et al. Eur J Med Chem. 2015 Mar 26;93:121-34. doi: 10.1016/j.ejmech.2015.01.063. Epub 2015 Feb 2. Eur J Med Chem. 2015. PMID: 25666912
Identification of novel, water-soluble, 2-amino-N-pyrimidin-4-yl acetamides as A2A receptor antagonists with in vivo efficacy.
Slee DH, Zhang X, Moorjani M, Lin E, Lanier MC, Chen Y, Rueter JK, Lechner SM, Markison S, Malany S, Joswig T, Santos M, Gross RS, Williams JP, Castro-Palomino JC, Crespo MI, Prat M, Gual S, Díaz JL, Wen J, O'Brien Z, Saunders J. Slee DH, et al. Among authors: gross rs. J Med Chem. 2008 Feb 14;51(3):400-6. doi: 10.1021/jm070623o. Epub 2008 Jan 12. J Med Chem. 2008. PMID: 18189346
2-Amino-N-pyrimidin-4-ylacetamides as A2A receptor antagonists: 2. Reduction of hERG activity, observed species selectivity, and structure-activity relationships.
Slee DH, Moorjani M, Zhang X, Lin E, Lanier MC, Chen Y, Rueter JK, Lechner SM, Markison S, Malany S, Joswig T, Santos M, Gross RS, Williams JP, Castro-Palomino JC, Crespo MI, Prat M, Gual S, Díaz JL, Jalali K, Sai Y, Zuo Z, Yang C, Wen J, O'Brien Z, Petroski R, Saunders J. Slee DH, et al. Among authors: gross rs. J Med Chem. 2008 Mar 27;51(6):1730-9. doi: 10.1021/jm701187w. Epub 2008 Feb 29. J Med Chem. 2008. PMID: 18307293
Design and synthesis of tricyclic imidazo[4,5-b]pyridin-2-ones as corticotropin-releasing factor-1 antagonists.
Guo Z, Tellew JE, Gross RS, Dyck B, Grey J, Haddach M, Kiankarimi M, Lanier M, Li BF, Luo Z, McCarthy JR, Moorjani M, Saunders J, Sullivan R, Zhang X, Zamani-Kord S, Grigoriadis DE, Crowe PD, Chen TK, Williams JP. Guo Z, et al. Among authors: gross rs. J Med Chem. 2005 Aug 11;48(16):5104-7. doi: 10.1021/jm050384+. J Med Chem. 2005. PMID: 16078829
Structure-kinetic relationships--an overlooked parameter in hit-to-lead optimization: a case of cyclopentylamines as chemokine receptor 2 antagonists.
Vilums M, Zweemer AJ, Yu Z, de Vries H, Hillger JM, Wapenaar H, Bollen IA, Barmare F, Gross R, Clemens J, Krenitsky P, Brussee J, Stamos D, Saunders J, Heitman LH, Ijzerman AP. Vilums M, et al. J Med Chem. 2013 Oct 10;56(19):7706-14. doi: 10.1021/jm4011737. Epub 2013 Sep 27. J Med Chem. 2013. PMID: 24028535
110 results