J
J C Quintero
Publications - 4
Citations - 1082
J C Quintero is an academic researcher. The author has contributed to research in topics: HIV Protease Inhibitor & Isostere. The author has an hindex of 4, co-authored 4 publications receiving 1057 citations.
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Journal ArticleDOI
L-735,524: an orally bioavailable human immunodeficiency virus type 1 protease inhibitor
Joseph P. Vacca,Bruce D. Dorsey,William A. Schleif,Rhonda B. Levin,Stacey L. McDaniel,Paul L. Darke,J Zugay,J C Quintero,O M Blahy,E Roth +9 more
TL;DR: L-735,524 is a potent inhibitor of virus replication in cell culture and inhibits the protease-mediated cleavage of the viral precursor polyproteins that results in the production of noninfectious progeny viral particles.
Journal ArticleDOI
L-735,524 : the design of a potent and orally bioavailable HIV protease inhibitor
Bruce D. Dorsey,Rhonda B. Levin,Stacey L. McDaniel,Joseph P. Vacca,J. P. Guare,Paul L. Darke,Zugay Ja,Emilio A. Emini,William A. Schleif,J C Quintero +9 more
TL;DR: The design of L-735,524, a potent and competitively inhibits HIV-1 PR and HIV-2 PR with Ki values of 0.52 and 3.3 nM, is guided by molecular modeling and an X-ray crystal structure of the inhibited enzyme complex, and is currently in phase II human clinical trials.
Journal ArticleDOI
Synthesis and antiviral activity of a series of HIV-1 protease inhibitors with functionality tethered to the P1 or P1' phenyl substituents: X-ray crystal structure assisted design.
Wayne J. Thompson,Paula M.D. Fitzgerald,Holloway Mk,Emilio A. Emini,Paul L. Darke,Brian M. McKeever,William A. Schleif,J C Quintero,Zugay Ja,Thomas J. Tucker +9 more
TL;DR: By tethering a polar hydrophilic group to the P1 or P1' substituent of a Phe-based hydroxyethylene isostere, the antiviral potency of a series of HIV protease inhibitors was improved and the optimum enhancement of anti-HIV activity was observed with the 4-morpholinylethoxy substituents.
Journal Article
HIV-1 protease inhibitors: synthesis and biological evaluation of glycopeptidemimetics.
Arun K. Ghosh,S. P. Mckee,W. M. Sanders,P. L. Darke,J. A. Zugay,Emilio A. Emini,W. A. Schleif,J C Quintero,J. R. Huff,Paul S. Anderson +9 more
TL;DR: A series of glycopeptidemimetics based on the hydroxyethylene Phe-Phe isostere have been synthesized and evaluated for their ability to inhibit the enzyme HIV-1 protease and compound 21 was the most potent inhibitor.