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83 results

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Page 1
Synthesis and SAR of 1,2,3,4-tetrahydroisoquinolin-1-ones as novel G-protein-coupled receptor 40 (GPR40) antagonists.
Humphries PS, Benbow JW, Bonin PD, Boyer D, Doran SD, Frisbie RK, Piotrowski DW, Balan G, Bechle BM, Conn EL, Dirico KJ, Oliver RM, Soeller WC, Southers JA, Yang X. Humphries PS, et al. Among authors: oliver rm. Bioorg Med Chem Lett. 2009 May 1;19(9):2400-3. doi: 10.1016/j.bmcl.2009.03.082. Epub 2009 Mar 25. Bioorg Med Chem Lett. 2009. PMID: 19346127
The discovery of novel calcium sensing receptor negative allosteric modulators.
Balan G, Bauman J, Bhattacharya S, Castrodad M, Healy DR, Herr M, Humphries P, Jennings S, Kalgutkar AS, Kapinos B, Khot V, Lazarra K, Li M, Li Y, Neagu C, Oliver R, Piotrowski DW, Price D, Qi H, Simmons HA, Southers J, Wei L, Zhang Y, Paralkar VM. Balan G, et al. Bioorg Med Chem Lett. 2009 Jun 15;19(12):3328-32. doi: 10.1016/j.bmcl.2009.04.044. Epub 2009 Apr 18. Bioorg Med Chem Lett. 2009. PMID: 19442519
Short-acting 5-(trifluoromethyl)pyrido[4,3-d]pyrimidin-4(3H)-one derivatives as orally-active calcium-sensing receptor antagonists.
Didiuk MT, Griffith DA, Benbow JW, Liu KK, Walker DP, Bi FC, Morris J, Guzman-Perez A, Gao H, Bechle BM, Kelley RM, Yang X, Dirico K, Ahmed S, Hungerford W, DiBrinno J, Zawistoski MP, Bagley SW, Li J, Zeng Y, Santucci S, Oliver R, Corbett M, Olson T, Chen C, Li M, Paralkar VM, Riccardi KA, Healy DR, Kalgutkar AS, Maurer TS, Nguyen HT, Frederick KS. Didiuk MT, et al. Among authors: oliver r. Bioorg Med Chem Lett. 2009 Aug 15;19(16):4555-9. doi: 10.1016/j.bmcl.2009.07.004. Epub 2009 Jul 8. Bioorg Med Chem Lett. 2009. PMID: 19625189
Metabolism-guided design of short-acting calcium-sensing receptor antagonists.
Southers JA, Bauman JN, Price DA, Humphries PS, Balan G, Sagal JF, Maurer TS, Zhang Y, Oliver R, Herr M, Healy DR, Li M, Kapinos B, Fate GD, Riccardi KA, Paralkar VM, Brown TA, Kalgutkar AS. Southers JA, et al. ACS Med Chem Lett. 2010 May 13;1(5):219-23. doi: 10.1021/ml100058w. eCollection 2010 Aug 12. ACS Med Chem Lett. 2010. PMID: 24900198 Free PMC article.
Discovery tactics to mitigate toxicity risks due to reactive metabolite formation with 2-(2-hydroxyaryl)-5-(trifluoromethyl)pyrido[4,3-d]pyrimidin-4(3h)-one derivatives, potent calcium-sensing receptor antagonists and clinical candidate(s) for the treatment of osteoporosis.
Kalgutkar AS, Griffith DA, Ryder T, Sun H, Miao Z, Bauman JN, Didiuk MT, Frederick KS, Zhao SX, Prakash C, Soglia JR, Bagley SW, Bechle BM, Kelley RM, Dirico K, Zawistoski M, Li J, Oliver R, Guzman-Perez A, Liu KK, Walker DP, Benbow JW, Morris J. Kalgutkar AS, et al. Among authors: oliver r. Chem Res Toxicol. 2010 Jun 21;23(6):1115-26. doi: 10.1021/tx100137n. Chem Res Toxicol. 2010. PMID: 20507089
Discovery of N-benzyl-2-[(4S)-4-(1H-indol-3-ylmethyl)-5-oxo-1-phenyl-4,5-dihydro-6H-[1,2,4]triazolo[4,3-a][1,5]benzodiazepin-6-yl]-N-isopropylacetamide, an orally active, gut-selective CCK1 receptor agonist for the potential treatment of obesity.
Elliott RL, Cameron KO, Chin JE, Bartlett JA, Beretta EE, Chen Y, Jardine Pda S, Dubins JS, Gillaspy ML, Hargrove DM, Kalgutkar AS, LaFlamme JA, Lame ME, Martin KA, Maurer TS, Nardone NA, Oliver RM, Scott DO, Sun D, Swick AG, Trebino CE, Zhang Y. Elliott RL, et al. Among authors: oliver rm. Bioorg Med Chem Lett. 2010 Nov 15;20(22):6797-801. doi: 10.1016/j.bmcl.2010.08.115. Epub 2010 Sep 28. Bioorg Med Chem Lett. 2010. PMID: 20851601
Potent inhibitors of LpxC for the treatment of Gram-negative infections.
Brown MF, Reilly U, Abramite JA, Arcari JT, Oliver R, Barham RA, Che Y, Chen JM, Collantes EM, Chung SW, Desbonnet C, Doty J, Doroski M, Engtrakul JJ, Harris TM, Huband M, Knafels JD, Leach KL, Liu S, Marfat A, Marra A, McElroy E, Melnick M, Menard CA, Montgomery JI, Mullins L, Noe MC, O'Donnell J, Penzien J, Plummer MS, Price LM, Shanmugasundaram V, Thoma C, Uccello DP, Warmus JS, Wishka DG. Brown MF, et al. J Med Chem. 2012 Jan 26;55(2):914-23. doi: 10.1021/jm2014748. Epub 2012 Jan 11. J Med Chem. 2012. PMID: 22175825
Trifluoromethylpyrimidine-based inhibitors of proline-rich tyrosine kinase 2 (PYK2): structure-activity relationships and strategies for the elimination of reactive metabolite formation.
Walker DP, Bi FC, Kalgutkar AS, Bauman JN, Zhao SX, Soglia JR, Aspnes GE, Kung DW, Klug-McLeod J, Zawistoski MP, McGlynn MA, Oliver R, Dunn M, Li JC, Richter DT, Cooper BA, Kath JC, Hulford CA, Autry CL, Luzzio MJ, Ung EJ, Roberts WG, Bonnette PC, Buckbinder L, Mistry A, Griffor MC, Han S, Guzman-Perez A. Walker DP, et al. Bioorg Med Chem Lett. 2008 Dec 1;18(23):6071-7. doi: 10.1016/j.bmcl.2008.10.030. Epub 2008 Oct 11. Bioorg Med Chem Lett. 2008. PMID: 18951788
83 results