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

Tao Jiang; Kelli L Kuhen; Karen Wolff; Hong Yin; Kimberly Bieza; Jeremy Caldwell; Badry Bursulaya; Tove Tuntland; Kanyin Zhang; Donald Karanewsky; Yun He

doi:10.1016/j.bmcl.2006.01.066

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

Bioorg Med Chem Lett. 2006 Apr 15;16(8):2109-12. doi: 10.1016/j.bmcl.2006.01.066. Epub 2006 Feb 7.

Authors

Tao Jiang¹, Kelli L Kuhen, Karen Wolff, Hong Yin, Kimberly Bieza, Jeremy Caldwell, Badry Bursulaya, Tove Tuntland, Kanyin Zhang, Donald Karanewsky, Yun He

Affiliation

¹ Genomics Institute of the Novartis Research Foundation (GNF), 10715 John Jay Hopkins Drive, San Diego, CA 92121, USA.

PMID: 16464578
DOI: 10.1016/j.bmcl.2006.01.066

Abstract

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.

Publication types

Evaluation Study

MeSH terms

Anti-HIV Agents / chemical synthesis
Anti-HIV Agents / pharmacology
Drug Design
Drug Resistance, Viral
HIV-1 / drug effects*
Indoles / chemical synthesis*
Indoles / pharmacokinetics*
Reverse Transcriptase Inhibitors / chemical synthesis*
Reverse Transcriptase Inhibitors / pharmacokinetics*
Stereoisomerism
Structure-Activity Relationship
Virus Replication / drug effects*

Substances

Anti-HIV Agents
Indoles
Reverse Transcriptase Inhibitors