Design, synthesis and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part I

A novel oxindole was discovered as an HIV non-nucleoside reverse transcriptase inhibitor via HTS using a cell-based assay. Systematic structural modifications were carried out to establish its SAR. These modifications led to the identification of oxindoles with low nanomolar potency for inhibiting H...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2006-04, Vol.16 (8), p.2105-2108
Main Authors: Jiang, Tao, Kuhen, Kelli L., Wolff, Karen, Yin, Hong, Bieza, Kimberly, Caldwell, Jeremy, Bursulaya, Badry, Wu, Tom Yao-Hsing, He, Yun
Format: Article
Language:English
Subjects:
AIDS
Anti-HIV Agents - chemical synthesis
Anti-HIV Agents - pharmacology
Antibiotics. Antiinfectious agents. Antiparasitic agents
Antiviral agents
Biological and medical sciences
Drug Resistance, Viral
HIV
HIV-1 - drug effects
Human immunodeficiency virus 1
Indoles - chemical synthesis
Indoles - pharmacology
Inhibitor
Medical sciences
Oxindole
Pharmacology. Drug treatments
Reverse transcriptase
Reverse Transcriptase Inhibitors - chemical synthesis
Reverse Transcriptase Inhibitors - pharmacology
SAR
Stereoisomerism
Structure-Activity Relationship
Virus Replication
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Summary:A novel oxindole was discovered as an HIV non-nucleoside reverse transcriptase inhibitor via HTS using a cell-based assay. Systematic structural modifications were carried out to establish its SAR. These modifications led to the identification of oxindoles with low nanomolar potency for inhibiting HIV replication. These novel and potent oxindoles could serve as advanced leads for further optimizations.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2006.01.073