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Page 1
Toward second generation hepatitis C virus NS3 serine protease inhibitors: discovery of novel P4 modified analogues with improved potency and pharmacokinetic profile.
Arasappan A, Padilla AI, Jao E, Bennett F, Bogen SL, Chen KX, Pike RE, Sannigrahi M, Soares J, Venkatraman S, Vibulbhan B, Saksena AK, Girijavallabhan V, Tong X, Cheng KC, Njoroge FG. Arasappan A, et al. Among authors: pike re. J Med Chem. 2009 May 14;52(9):2806-17. doi: 10.1021/jm801616e. J Med Chem. 2009. PMID: 19371095
Discovery of Narlaprevir (SCH 900518): A Potent, Second Generation HCV NS3 Serine Protease Inhibitor.
Arasappan A, Bennett F, Bogen SL, Venkatraman S, Blackman M, Chen KX, Hendrata S, Huang Y, Huelgas RM, Nair L, Padilla AI, Pan W, Pike R, Pinto P, Ruan S, Sannigrahi M, Velazquez F, Vibulbhan B, Wu W, Yang W, Saksena AK, Girijavallabhan V, Shih NY, Kong J, Meng T, Jin Y, Wong J, McNamara P, Prongay A, Madison V, Piwinski JJ, Cheng KC, Morrison R, Malcolm B, Tong X, Ralston R, Njoroge FG. Arasappan A, et al. ACS Med Chem Lett. 2010 Feb 15;1(2):64-9. doi: 10.1021/ml9000276. eCollection 2010 May 13. ACS Med Chem Lett. 2010. PMID: 24900178 Free PMC article.
Hepatitis C virus NS3-4A serine protease inhibitors: SAR of P'2 moiety with improved potency.
Arasappan A, Njoroge FG, Chan TY, Bennett F, Bogen SL, Chen K, Gu H, Hong L, Jao E, Liu YT, Lovey RG, Parekh T, Pike RE, Pinto P, Santhanam B, Venkatraman S, Vaccaro H, Wang H, Yang X, Zhu Z, Mckittrick B, Saksena AK, Girijavallabhan V, Pichardo J, Butkiewicz N, Ingram R, Malcolm B, Prongay A, Yao N, Marten B, Madison V, Kemp S, Levy O, Lim-Wilby M, Tamura S, Ganguly AK. Arasappan A, et al. Among authors: pike re. Bioorg Med Chem Lett. 2005 Oct 1;15(19):4180-4. doi: 10.1016/j.bmcl.2005.06.091. Bioorg Med Chem Lett. 2005. PMID: 16087332
Posaconazole (Noxafil, SCH 56592), a new azole antifungal drug, was a discovery based on the isolation and mass spectral characterization of a circulating metabolite of an earlier lead (SCH 51048).
Nomeir AA, Pramanik BN, Heimark L, Bennett F, Veals J, Bartner P, Hilbert M, Saksena A, McNamara P, Girijavallabhan V, Ganguly AK, Lovey R, Pike R, Wang H, Liu YT, Kumari P, Korfmacher W, Lin CC, Cacciapuoti A, Loebenberg D, Hare R, Miller G, Pickett C. Nomeir AA, et al. J Mass Spectrom. 2008 Apr;43(4):509-17. doi: 10.1002/jms.1341. J Mass Spectrom. 2008. PMID: 18059003
Discovery of SCH446211 (SCH6): a new ketoamide inhibitor of the HCV NS3 serine protease and HCV subgenomic RNA replication.
Bogen SL, Arasappan A, Bennett F, Chen K, Jao E, Liu YT, Lovey RG, Venkatraman S, Pan W, Parekh T, Pike RE, Ruan S, Liu R, Baroudy B, Agrawal S, Chase R, Ingravallo P, Pichardo J, Prongay A, Brisson JM, Hsieh TY, Cheng KC, Kemp SJ, Levy OE, Lim-Wilby M, Tamura SY, Saksena AK, Girijavallabhan V, Njoroge FG. Bogen SL, et al. Among authors: pike re. J Med Chem. 2006 May 4;49(9):2750-7. doi: 10.1021/jm060077j. J Med Chem. 2006. PMID: 16640336
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