Design, synthesis, and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part 2

A series of heterocycle-containing oxindoles was synthesized and their HIV antiviral activities were assessed. Some of these analogs exhibited potent inhibitory activities against both wild-type virus and a number of drug-resistant mutant viruses. In addition, oxindole 9z also showed promising pharm...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2006-04, Vol.16 (8), p.2109-2112
Hauptverfasser:	Jiang, Tao, Kuhen, Kelli L., Wolff, Karen, Yin, Hong, Bieza, Kimberly, Caldwell, Jeremy, Bursulaya, Badry, Tuntland, Tove, Zhang, Kanyin, Karanewsky, Donald, He, Yun
Format:	Artikel
Sprache:	eng
Schlagworte:	AIDS Anti-HIV Agents - chemical synthesis Anti-HIV Agents - pharmacology Antibiotics. Antiinfectious agents. Antiparasitic agents Antiviral agents Biological and medical sciences Drug Design Drug Resistance, Viral Heterocycle HIV HIV-1 - drug effects Human immunodeficiency virus 1 Indoles - chemical synthesis Indoles - pharmacokinetics Inhibitor Medical sciences Oxindole Pharmacology. Drug treatments Reverse transcriptase Reverse Transcriptase Inhibitors - chemical synthesis Reverse Transcriptase Inhibitors - pharmacokinetics SAR Stereoisomerism Structure-Activity Relationship Virus Replication - drug effects
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Zusammenfassung:	A series of heterocycle-containing oxindoles was synthesized and their HIV antiviral activities were assessed. Some of these analogs exhibited potent inhibitory activities against both wild-type virus and a number of drug-resistant mutant viruses. In addition, oxindole 9z also showed promising pharmacokinetics.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2006.01.066