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Page 1
Lead Optimization to Advance Protease-Activated Receptor-1 Antagonists in Early Discovery.
Mandal M, Madeira M, Amin RP, Buevich AV, Cheng A, Labroli M, Liu X, Acton J, Pio B, Basso A, Chobanian H, Dong G, Dropinski J, Guo Y, Guo Z, Kurowski S, Korfmacher W, Lee S, Meng D, Ondeyka D, Yang Z, Zhang R, Wei H, Wu Z, Zhang F, Wollenberg G, Biftu T, Greenlee WJ, Chintala M, Maletic M, Zhu Z. Mandal M, et al. Among authors: guo y, guo z. J Med Chem. 2022 Apr 14;65(7):5575-5592. doi: 10.1021/acs.jmedchem.1c02048. Epub 2022 Mar 29. J Med Chem. 2022. PMID: 35349275
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.
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 (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 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: guo z. J Med Chem. 2007 May 17;50(10):2310-8. doi: 10.1021/jm060173k. Epub 2007 Apr 20. J Med Chem. 2007. PMID: 17444623
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.
Discovery of novel hydroxamates as highly potent tumor necrosis factor-alpha converting enzyme inhibitors. Part II: optimization of the S3' pocket.
Mazzola RD Jr, Zhu Z, Sinning L, McKittrick B, Lavey B, Spitler J, Kozlowski J, Neng-Yang S, Zhou G, Guo Z, Orth P, Madison V, Sun J, Lundell D, Niu X. Mazzola RD Jr, et al. Among authors: guo z. Bioorg Med Chem Lett. 2008 Nov 1;18(21):5809-14. doi: 10.1016/j.bmcl.2008.09.045. Epub 2008 Sep 13. Bioorg Med Chem Lett. 2008. PMID: 18835710
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: guo z. J Med Chem. 2009 Jun 25;52(12):3679-88. doi: 10.1021/jm801632a. J Med Chem. 2009. PMID: 19456105
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