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Page 1
Rational design of a novel, potent, and orally bioavailable cyclohexylamine DPP-4 inhibitor by application of molecular modeling and X-ray crystallography of sitagliptin.
Biftu T, Scapin G, Singh S, Feng D, Becker JW, Eiermann G, He H, Lyons K, Patel S, Petrov A, Sinha-Roy R, Zhang B, Wu J, Zhang X, Doss GA, Thornberry NA, Weber AE. Biftu T, et al. Among authors: scapin g. Bioorg Med Chem Lett. 2007 Jun 15;17(12):3384-7. doi: 10.1016/j.bmcl.2007.03.095. Epub 2007 Apr 2. Bioorg Med Chem Lett. 2007. PMID: 17433672
Design and synthesis of potent, orally bioavailable dihydroquinazolinone inhibitors of p38 MAP kinase.
Stelmach JE, Liu L, Patel SB, Pivnichny JV, Scapin G, Singh S, Hop CE, Wang Z, Strauss JR, Cameron PM, Nichols EA, O'Keefe SJ, O'Neill EA, Schmatz DM, Schwartz CD, Thompson CM, Zaller DM, Doherty JB. Stelmach JE, et al. Among authors: scapin g. Bioorg Med Chem Lett. 2003 Jan 20;13(2):277-80. doi: 10.1016/s0960-894x(02)00752-7. Bioorg Med Chem Lett. 2003. PMID: 12482439
Hybrid-designed inhibitors of p38 MAP kinase utilizing N-arylpyridazinones.
Colletti SL, Frie JL, Dixon EC, Singh SB, Choi BK, Scapin G, Fitzgerald CE, Kumar S, Nichols EA, O'Keefe SJ, O'Neill EA, Porter G, Samuel K, Schmatz DM, Schwartz CD, Shoop WL, Thompson CM, Thompson JE, Wang R, Woods A, Zaller DM, Doherty JB. Colletti SL, et al. Among authors: scapin g. J Med Chem. 2003 Jan 30;46(3):349-52. doi: 10.1021/jm025585h. J Med Chem. 2003. PMID: 12540232
Discovery of potent, selective, and orally bioavailable oxadiazole-based dipeptidyl peptidase IV inhibitors.
Xu J, Wei L, Mathvink RJ, Edmondson SD, Eiermann GJ, He H, Leone JF, Leiting B, Lyons KA, Marsilio F, Patel RA, Patel SB, Petrov A, Scapin G, Wu JK, Thornberry NA, Weber AE. Xu J, et al. Among authors: scapin g. Bioorg Med Chem Lett. 2006 Oct 15;16(20):5373-7. doi: 10.1016/j.bmcl.2006.07.061. Epub 2006 Aug 17. Bioorg Med Chem Lett. 2006. PMID: 16919457
(3R)-4-[(3R)-3-Amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-(2,2,2-trifluoroethyl)-1,4-diazepan-2-one, a selective dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes.
Biftu T, Feng D, Qian X, Liang GB, Kieczykowski G, Eiermann G, He H, Leiting B, Lyons K, Petrov A, Sinha-Roy R, Zhang B, Scapin G, Patel S, Gao YD, Singh S, Wu J, Zhang X, Thornberry NA, Weber AE. Biftu T, et al. Among authors: scapin g. Bioorg Med Chem Lett. 2007 Jan 1;17(1):49-52. doi: 10.1016/j.bmcl.2006.09.099. Epub 2006 Oct 5. Bioorg Med Chem Lett. 2007. PMID: 17055272
4-aminophenylalanine and 4-aminocyclohexylalanine derivatives as potent, selective, and orally bioavailable inhibitors of dipeptidyl peptidase IV.
Duffy JL, Kirk BA, Wang L, Eiermann GJ, He H, Leiting B, Lyons KA, Patel RA, Patel SB, Petrov A, Scapin G, Wu JK, Thornberry NA, Weber AE. Duffy JL, et al. Among authors: scapin g. Bioorg Med Chem Lett. 2007 May 15;17(10):2879-85. doi: 10.1016/j.bmcl.2007.02.066. Epub 2007 Feb 25. Bioorg Med Chem Lett. 2007. PMID: 17350841
105 results