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Discovery of MK-8831, A Novel Spiro-Proline Macrocycle as a Pan-Genotypic HCV-NS3/4a Protease Inhibitor.
Neelamkavil SF, Agrawal S, Bara T, Bennett C, Bhat S, Biswas D, Brockunier L, Buist N, Burnette D, Cartwright M, Chackalamannil S, Chase R, Chelliah M, Chen A, Clasby M, Colandrea VJ, Davies IW, Eagen K, Guo Z, Han Y, Howe J, Jayne C, Josien H, Kargman S, Marcantonio K, Miao S, Miller R, Nolting A, Pinto P, Rajagopalan M, Ruck RT, Shah U, Soriano A, Sperbeck D, Velazquez F, Wu J, Xia Y, Venkatraman S. Neelamkavil SF, et al. Among authors: guo z. ACS Med Chem Lett. 2015 Dec 22;7(1):111-6. doi: 10.1021/acsmedchemlett.5b00425. eCollection 2016 Jan 14. ACS Med Chem Lett. 2015. PMID: 26819676 Free PMC article.
Novel Quinoline-Based P2-P4 Macrocyclic Derivatives As Pan-Genotypic HCV NS3/4a Protease Inhibitors.
Shah U, Jayne C, Chackalamannil S, Velázquez F, Guo Z, Buevich A, Howe JA, Chase R, Soriano A, Agrawal S, Rudd MT, McCauley JA, Liverton NJ, Romano J, Bush K, Coleman PJ, Grisé-Bard C, Brochu MC, Charron S, Aulakh V, Bachand B, Beaulieu P, Zaghdane H, Bhat S, Han Y, Vacca JP, Davies IW, Weber AE, Venkatraman S. Shah U, et al. Among authors: guo z. ACS Med Chem Lett. 2014 Jan 9;5(3):264-9. doi: 10.1021/ml400466p. eCollection 2014 Mar 13. ACS Med Chem Lett. 2014. PMID: 24900818 Free PMC article.
Himbacine-derived thrombin receptor antagonists: c7-spirocyclic analogues of vorapaxar.
Chelliah MV, Eagen K, Guo Z, Chackalamannil S, Xia Y, Tsai H, Greenlee WJ, Ahn HS, Kurowski S, Boykow G, Hsieh Y, Chintala M. Chelliah MV, et al. Among authors: guo z. ACS Med Chem Lett. 2014 Mar 11;5(5):561-5. doi: 10.1021/ml500008w. eCollection 2014 May 8. ACS Med Chem Lett. 2014. PMID: 24900880 Free PMC article.
Design and Synthesis of P2-P4 Macrocycles Containing a Unique Spirocyclic Proline: A New Class of HCV NS3/4A Inhibitors.
Velázquez F, Chelliah M, Clasby M, Guo Z, Howe J, Miller R, Neelamkavil S, Shah U, Soriano A, Xia Y, Venkatraman S, Chackalamannil S, Davies IW. Velázquez F, et al. Among authors: guo z. ACS Med Chem Lett. 2016 Oct 17;7(12):1173-1178. doi: 10.1021/acsmedchemlett.6b00321. eCollection 2016 Dec 8. ACS Med Chem Lett. 2016. PMID: 27994759 Free PMC article.
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: guo z. J Med Chem. 2006 Oct 5;49(20):6074-86. doi: 10.1021/jm060325b. J Med Chem. 2006. PMID: 17004721
Discovery of hydroxy pyrimidine Factor IXa inhibitors.
Jayne CL, Andreani T, Chan TY, Chelliah MV, Clasby MC, Dwyer M, Eagen KA, Fried S, Greenlee WJ, Guo Z, Hawes B, Hruza A, Ingram R, Keertikar KM, Neelamkavil S, Reichert P, Xia Y, Chackalamannil S. Jayne CL, et al. Among authors: guo z. Bioorg Med Chem Lett. 2020 Aug 1;30(15):127279. doi: 10.1016/j.bmcl.2020.127279. Epub 2020 May 23. Bioorg Med Chem Lett. 2020. PMID: 32527459
Discovery of potent sulfonamide P4-capped ketoamide second generation inhibitors of hepatitis C virus NS3 serine protease with favorable pharmacokinetic profiles in preclinical species.
Bogen SL, Arasappan A, Velazquez F, Blackman M, Huelgas R, Pan W, Siegel E, Nair LG, Venkatraman S, Guo Z, Doll R, Shih NY, Njoroge FG. Bogen SL, et al. Among authors: guo z. Bioorg Med Chem. 2010 Mar 1;18(5):1854-65. doi: 10.1016/j.bmc.2010.01.044. Epub 2010 Jan 25. Bioorg Med Chem. 2010. PMID: 20149666
The introduction of P4 substituted 1-methylcyclohexyl groups into Boceprevir: a change in direction in the search for a second generation HCV NS3 protease inhibitor.
Bennett F, Huang Y, Hendrata S, Lovey R, Bogen SL, Pan W, Guo Z, Prongay A, Chen KX, Arasappan A, Venkatraman S, Velazquez F, Nair L, Sannigrahi M, Tong X, Pichardo J, Cheng KC, Girijavallabhan VM, Saksena AK, Njoroge FG. Bennett F, et al. Among authors: guo z. Bioorg Med Chem Lett. 2010 Apr 15;20(8):2617-21. doi: 10.1016/j.bmcl.2010.02.063. Epub 2010 Feb 19. Bioorg Med Chem Lett. 2010. PMID: 20303756
Design and synthesis of novel proline based factor XIa selective inhibitors as leads for potential new anticoagulants.
Hussain Z, Cooke AJ, Neelamkavil S, Brown L, Carswell E, Geissler WM, Guo Z, Hawes B, Kelly TM, Kiyoi Y, Lai K, Lesburg C, Pow E, Zang Y, Wood HB, Edmondson SD, Liu W. Hussain Z, et al. Among authors: guo z. Bioorg Med Chem Lett. 2020 Aug 15;30(16):127072. doi: 10.1016/j.bmcl.2020.127072. Epub 2020 Feb 29. Bioorg Med Chem Lett. 2020. PMID: 32340773
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