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Discovery of an oxybenzylglycine based peroxisome proliferator activated receptor alpha selective agonist 2-((3-((2-(4-chlorophenyl)-5-methyloxazol-4-yl)methoxy)benzyl)(methoxycarbonyl)amino)acetic acid (BMS-687453).
Li J, Kennedy LJ, Shi Y, Tao S, Ye XY, Chen SY, Wang Y, Hernández AS, Wang W, Devasthale PV, Chen S, Lai Z, Zhang H, Wu S, Smirk RA, Bolton SA, Ryono DE, Zhang H, Lim NK, Chen BC, Locke KT, O'Malley KM, Zhang L, Srivastava RA, Miao B, Meyers DS, Monshizadegan H, Search D, Grimm D, Zhang R, Harrity T, Kunselman LK, Cap M, Kadiyala P, Hosagrahara V, Zhang L, Xu C, Li YX, Muckelbauer JK, Chang C, An Y, Krystek SR, Blanar MA, Zahler R, Mukherjee R, Cheng PT, Tino JA. Li J, et al. Among authors: bolton sa. J Med Chem. 2010 Apr 8;53(7):2854-64. doi: 10.1021/jm9016812. J Med Chem. 2010. PMID: 20218621
Discovery of a Partial Glucokinase Activator Clinical Candidate: Diethyl ((3-(3-((5-(Azetidine-1-carbonyl)pyrazin-2-yl)oxy)-5-isopropoxybenzamido)-1H-pyrazol-1-yl)methyl)phosphonate (BMS-820132).
Shi Y, Wang Y, Meng W, Brigance RP, Ryono DE, Bolton S, Zhang H, Chen S, Smirk R, Tao S, Tino JA, Williams KN, Sulsky R, Nielsen L, Ellsworth B, Wong MKY, Sun JH, Leith LW, Sun D, Wu DR, Gupta A, Rampulla R, Mathur A, Chen BC, Wang A, Fuentes-Catanio HG, Kunselman L, Cap M, Zalaznick J, Ma X, Liu H, Taylor JR, Zebo R, Jones B, Kalinowski S, Swartz J, Staal A, O'Malley K, Kopcho L, Muckelbauer JK, Krystek SR Jr, Spronk SA, Marcinkeviciene J, Everlof G, Chen XQ, Xu C, Li YX, Langish RA, Yang Y, Wang Q, Behnia K, Fura A, Janovitz EB, Pannacciulli N, Griffen S, Zinker BA, Krupinski J, Kirby M, Whaley J, Zahler R, Barrish JC, Robl JA, Cheng PTW. Shi Y, et al. Among authors: bolton s. J Med Chem. 2022 Mar 10;65(5):4291-4317. doi: 10.1021/acs.jmedchem.1c02110. Epub 2022 Feb 18. J Med Chem. 2022. PMID: 35179904
Discovery of nonbenzamidine factor VIIa inhibitors using a biaryl acid scaffold.
Bolton SA, Sutton JC, Anumula R, Bisacchi GS, Jacobson B, Slusarchyk WA, Treuner UD, Wu SC, Zhao G, Pi Z, Sheriff S, Smirk RA, Bisaha S, Cheney DL, Wei A, Schumacher WA, Hartl KS, Liu E, Zahler R, Seiler SM. Bolton SA, et al. Bioorg Med Chem Lett. 2013 Sep 15;23(18):5239-43. doi: 10.1016/j.bmcl.2013.06.028. Epub 2013 Jun 20. Bioorg Med Chem Lett. 2013. PMID: 23927973
Synthesis and SAR of 4-carboxy-2-azetidinone mechanism-based tryptase inhibitors.
Sutton JC, Bolton SA, Hartl KS, Huang MH, Jacobs G, Meng W, Ogletree ML, Pi Z, Schumacher WA, Seiler SM, Slusarchyk WA, Treuner U, Zahler R, Zhao G, Bisacchi GS. Sutton JC, et al. Among authors: bolton sa. Bioorg Med Chem Lett. 2002 Nov 4;12(21):3229-33. doi: 10.1016/s0960-894x(02)00688-1. Bioorg Med Chem Lett. 2002. PMID: 12372540
Synthesis of potent and highly selective inhibitors of human tryptase.
Slusarchyk WA, Bolton SA, Hartl KS, Huang MH, Jacobs G, Meng W, Ogletree ML, Pi Z, Schumacher WA, Seiler SM, Sutton JC, Treuner U, Zahler R, Zhao G, Bisacchi GS. Slusarchyk WA, et al. Among authors: bolton sa. Bioorg Med Chem Lett. 2002 Nov 4;12(21):3235-8. doi: 10.1016/s0960-894x(02)00689-3. Bioorg Med Chem Lett. 2002. PMID: 12372541
Potent non-nitrile dipeptidic dipeptidyl peptidase IV inhibitors.
Simpkins LM, Bolton S, Pi Z, Sutton JC, Kwon C, Zhao G, Magnin DR, Augeri DJ, Gungor T, Rotella DP, Sun Z, Liu Y, Slusarchyk WS, Marcinkeviciene J, Robertson JG, Wang A, Robl JA, Atwal KS, Zahler RL, Parker RA, Kirby MS, Hamann LG. Simpkins LM, et al. Bioorg Med Chem Lett. 2007 Dec 1;17(23):6476-80. doi: 10.1016/j.bmcl.2007.09.090. Epub 2007 Oct 1. Bioorg Med Chem Lett. 2007. PMID: 17937986
11 results