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The discovery of asunaprevir (BMS-650032), an orally efficacious NS3 protease inhibitor for the treatment of hepatitis C virus infection.
Scola PM, Sun LQ, Wang AX, Chen J, Sin N, Venables BL, Sit SY, Chen Y, Cocuzza A, Bilder DM, D'Andrea SV, Zheng B, Hewawasam P, Tu Y, Friborg J, Falk P, Hernandez D, Levine S, Chen C, Yu F, Sheaffer AK, Zhai G, Barry D, Knipe JO, Han YH, Schartman R, Donoso M, Mosure K, Sinz MW, Zvyaga T, Good AC, Rajamani R, Kish K, Tredup J, Klei HE, Gao Q, Mueller L, Colonno RJ, Grasela DM, Adams SP, Loy J, Levesque PC, Sun H, Shi H, Sun L, Warner W, Li D, Zhu J, Meanwell NA, McPhee F. Scola PM, et al. Among authors: zhai g. J Med Chem. 2014 Mar 13;57(5):1730-52. doi: 10.1021/jm500297k. Epub 2014 Mar 5. J Med Chem. 2014. PMID: 24564672
Preclinical Profile and Characterization of the Hepatitis C Virus NS3 Protease Inhibitor Asunaprevir (BMS-650032).
McPhee F, Sheaffer AK, Friborg J, Hernandez D, Falk P, Zhai G, Levine S, Chaniewski S, Yu F, Barry D, Chen C, Lee MS, Mosure K, Sun LQ, Sinz M, Meanwell NA, Colonno RJ, Knipe J, Scola P. McPhee F, et al. Among authors: zhai g. Antimicrob Agents Chemother. 2012 Oct;56(10):5387-96. doi: 10.1128/AAC.01186-12. Epub 2012 Aug 6. Antimicrob Agents Chemother. 2012. PMID: 22869577 Free PMC article.
Discovery and early clinical evaluation of BMS-605339, a potent and orally efficacious tripeptidic acylsulfonamide NS3 protease inhibitor for the treatment of hepatitis C virus infection.
Scola PM, Wang AX, Good AC, Sun LQ, Combrink KD, Campbell JA, Chen J, Tu Y, Sin N, Venables BL, Sit SY, Chen Y, Cocuzza A, Bilder DM, D'Andrea S, Zheng B, Hewawasam P, Ding M, Thuring J, Li J, Hernandez D, Yu F, Falk P, Zhai G, Sheaffer AK, Chen C, Lee MS, Barry D, Knipe JO, Li W, Han YH, Jenkins S, Gesenberg C, Gao Q, Sinz MW, Santone KS, Zvyaga T, Rajamani R, Klei HE, Colonno RJ, Grasela DM, Hughes E, Chien C, Adams S, Levesque PC, Li D, Zhu J, Meanwell NA, McPhee F. Scola PM, et al. Among authors: zhai g. J Med Chem. 2014 Mar 13;57(5):1708-29. doi: 10.1021/jm401840s. Epub 2014 Feb 20. J Med Chem. 2014. PMID: 24555570
Functionalized triazines as potent HCV entry inhibitors.
Mull ES, Sun LQ, Zhao Q, Eggers B, Pokornowski K, Zhai G, Rajamani R, Jenkins S, Kramer M, Wang YK, Fang H, Tenney D, Baldick CJ, Cockett MI, Meanwell NA, Scola PM. Mull ES, et al. Among authors: zhai g. Bioorg Med Chem Lett. 2017 Feb 15;27(4):1089-1093. doi: 10.1016/j.bmcl.2016.12.038. Epub 2016 Dec 18. Bioorg Med Chem Lett. 2017. PMID: 28089701
P3-P4 ureas and reverse carbamates as potent HCV NS3 protease inhibitors: Effective transposition of the P4 hydrogen bond donor.
Venables BL, Sin N, Wang AX, Sun LQ, Tu Y, Hernandez D, Sheaffer A, Lee M, Dunaj C, Zhai G, Barry D, Friborg J, Yu F, Knipe J, Sandquist J, Falk P, Parker D, Good AC, Rajamani R, McPhee F, Meanwell NA, Scola PM. Venables BL, et al. Among authors: zhai g. Bioorg Med Chem Lett. 2018 Jun 1;28(10):1853-1859. doi: 10.1016/j.bmcl.2018.04.009. Epub 2018 Apr 5. Bioorg Med Chem Lett. 2018. PMID: 29650290
A novel small molecule inhibitor of hepatitis C virus entry.
Baldick CJ, Wichroski MJ, Pendri A, Walsh AW, Fang J, Mazzucco CE, Pokornowski KA, Rose RE, Eggers BJ, Hsu M, Zhai W, Zhai G, Gerritz SW, Poss MA, Meanwell NA, Cockett MI, Tenney DJ. Baldick CJ, et al. Among authors: zhai w, zhai g. PLoS Pathog. 2010 Sep 2;6(9):e1001086. doi: 10.1371/journal.ppat.1001086. PLoS Pathog. 2010. PMID: 20838466 Free PMC article.
938 results