Design and synthesis of novel HIV-1 protease inhibitors incorporating oxyindoles as the P 2 ′ -ligands

A series of novel oxyindole-derived HIV-1 protease inhibitors were designed and synthesized. A number of inhibitors exhibited low nanomolar inhibitory potencies against HIV protease. A series of novel oxyindole-derived HIV-1 protease inhibitors were designed and synthesized based upon our X-ray crys...

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Bibliographic Details
Published inBioorganic & medicinal chemistry letters Vol. 16; no. 7; pp. 1869 - 1873
Main Authors Ghosh, Arun K., Schiltz, Gary, Perali, Ramu Sridhar, Leshchenko, Sofiya, Kay, Stephanie, Walters, D. Eric, Koh, Yasuhiro, Maeda, Kenji, Mitsuya, Hiroaki
Format Journal Article
LanguageEnglish
Published Elsevier Ltd 01.04.2006
Subjects
Design
HIV proptease
Inhibitors
Oxyindole
Synthesis
TMC-114
Design
Inhibitors
Synthesis
HIV proptease
TMC-114
Oxyindole
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Summary:A series of novel oxyindole-derived HIV-1 protease inhibitors were designed and synthesized. A number of inhibitors exhibited low nanomolar inhibitory potencies against HIV protease. A series of novel oxyindole-derived HIV-1 protease inhibitors were designed and synthesized based upon our X-ray crystal structure of inhibitor 2 (TMC-114) bound to HIV-1 protease. The effects of substituents, spirocyclic rings, and ring sizes have been investigated. A number of inhibitors exhibited low nanomolar inhibitory potencies against HIV protease.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2006.01.011