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Page 1
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: jao e. 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
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: jao e. J Med Chem. 2006 May 4;49(9):2750-7. doi: 10.1021/jm060077j. J Med Chem. 2006. PMID: 16640336
Discovery of (1R,5S)-N-[3-amino-1-(cyclobutylmethyl)-2,3-dioxopropyl]- 3-[2(S)-[[[(1,1-dimethylethyl)amino]carbonyl]amino]-3,3-dimethyl-1-oxobutyl]- 6,6-dimethyl-3-azabicyclo[3.1.0]hexan-2(S)-carboxamide (SCH 503034), a selective, potent, orally bioavailable hepatitis C virus NS3 protease inhibitor: a potential therapeutic agent for the treatment of hepatitis C infection.
Venkatraman S, Bogen SL, Arasappan A, Bennett F, Chen K, Jao E, Liu YT, Lovey R, Hendrata S, Huang Y, Pan W, Parekh T, Pinto P, Popov V, Pike R, Ruan S, Santhanam B, Vibulbhan B, Wu W, Yang W, Kong J, Liang X, Wong J, Liu R, Butkiewicz N, Chase R, Hart A, Agrawal S, Ingravallo P, Pichardo J, Kong R, Baroudy B, Malcolm B, Guo Z, Prongay A, Madison V, Broske L, Cui X, Cheng KC, Hsieh Y, Brisson JM, Prelusky D, Korfmacher W, White R, Bogdanowich-Knipp S, Pavlovsky A, Bradley P, Saksena AK, Ganguly A, Piwinski J, Girijavallabhan V, Njoroge FG. Venkatraman S, et al. Among authors: jao e. J Med Chem. 2006 Oct 5;49(20):6074-86. doi: 10.1021/jm060325b. J Med Chem. 2006. PMID: 17004721
Discovery of the HCV NS3/4A protease inhibitor (1R,5S)-N-[3-amino-1-(cyclobutylmethyl)-2,3-dioxopropyl]-3- [2(S)-[[[(1,1-dimethylethyl)amino]carbonyl]amino]-3,3-dimethyl-1-oxobutyl]- 6,6-dimethyl-3-azabicyclo[3.1.0]hexan-2(S)-carboxamide (Sch 503034) II. Key steps in structure-based optimization.
Prongay AJ, Guo Z, Yao N, Pichardo J, Fischmann T, Strickland C, Myers J Jr, Weber PC, Beyer BM, Ingram R, Hong Z, Prosise WW, Ramanathan L, Taremi SS, Yarosh-Tomaine T, Zhang R, Senior M, Yang RS, Malcolm B, Arasappan A, Bennett F, Bogen SL, Chen K, Jao E, Liu YT, Lovey RG, Saksena AK, Venkatraman S, Girijavallabhan V, Njoroge FG, Madison V. Prongay AJ, et al. Among authors: jao e. J Med Chem. 2007 May 17;50(10):2310-8. doi: 10.1021/jm060173k. Epub 2007 Apr 20. J Med Chem. 2007. PMID: 17444623
Key steps in the structure-based optimization of the hepatitis C virus NS3/4A protease inhibitor SCH503034.
Madison V, Prongay AJ, Guo Z, Yao N, Pichardo J, Fischmann T, Strickland C, Myers J Jr, Weber PC, Beyer BM, Ingram R, Hong Z, Prosise WW, Ramanathan L, Taremi SS, Yarosh-Tomaine T, Zhang R, Senior M, Yang RS, Malcolm B, Arasappan A, Bennett F, Bogen SL, Chen K, Jao E, Liu YT, Lovey RG, Saksena AK, Venkatraman S, Girijavallabhan V, Njoroge FG. Madison V, et al. Among authors: jao e. J Synchrotron Radiat. 2008 May;15(Pt 3):204-7. doi: 10.1107/S0909049507064229. Epub 2008 Apr 18. J Synchrotron Radiat. 2008. PMID: 18421139 Free PMC article.
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: jao e. J Med Chem. 2009 May 14;52(9):2806-17. doi: 10.1021/jm801616e. J Med Chem. 2009. PMID: 19371095
Toward the back-up of boceprevir (SCH 503034): discovery of new extended P4-capped ketoamide inhibitors of hepatitis C virus NS3 serine protease with improved potency and pharmacokinetic profiles.
Bogen SL, Pan W, Ruan S, Nair LG, Arasappan A, Bennett F, Chen KX, Jao E, Venkatraman S, Vibulbhan B, Liu R, Cheng KC, Guo Z, Tong X, Saksena AK, Girijavallabhan V, Njoroge FG. Bogen SL, et al. Among authors: jao e. J Med Chem. 2009 Jun 25;52(12):3679-88. doi: 10.1021/jm801632a. J Med Chem. 2009. PMID: 19456105
Hydroxylated analogues of the orally active broad spectrum antifungal, Sch 51048 (1), and the discovery of posaconazole [Sch 56592; 2 or (S,S)-5].
Bennett F, Saksena AK, Lovey RG, Liu YT, Patel NM, Pinto P, Pike R, Jao E, Girijavallabhan VM, Ganguly AK, Loebenberg D, Wang H, Cacciapuoti A, Moss E, Menzel F, Hare RS, Nomeir A. Bennett F, et al. Among authors: jao e. Bioorg Med Chem Lett. 2006 Jan 1;16(1):186-90. doi: 10.1016/j.bmcl.2005.09.031. Epub 2005 Nov 2. Bioorg Med Chem Lett. 2006. PMID: 16260134
12 results