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 pharmacokinetics.
Jiang
Tao
T
Genomics Institute of the Novartis Research Foundation (GNF), 10715 John Jay Hopkins Drive, San Diego, CA 92121, USA.
Kuhen
Kelli L
KL
Wolff
Karen
K
Yin
Hong
H
Bieza
Kimberly
K
Caldwell
Jeremy
J
Bursulaya
Badry
B
Tuntland
Tove
T
Zhang
Kanyin
K
Karanewsky
Donald
D
He
Yun
Y
D019380:Anti-HIV Agents / Q000138:chemical synthesis / Q000494:pharmacology; D015195:Drug Design; D024882:Drug Resistance, Viral; D015497:HIV-1 / Q000187:drug effects*; D007211:Indoles / Q000138:chemical synthesis* / Q000493:pharmacokinetics*; D018894:Reverse Transcriptase Inhibitors / Q000138:chemical synthesis* / Q000493:pharmacokinetics*; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D014779:Virus Replication / Q000187:drug effects*
D019380:Anti-HIV Agents; D007211:Indoles; D018894:Reverse Transcriptase Inhibitors