THIAZOLOBENZIMIDAZOLES--A NEW CLASS OF ANTI-HIV AGENTS (MEETING ABSTRACT)

Important note: Information in this article was accurate in 1992. The state of the art may have changed since the publication date.

THIAZOLOBENZIMIDAZOLES--A NEW CLASS OF ANTI-HIV AGENTS (MEETING ABSTRACT)

Proc Annu Meet Am Assoc Cancer Res; 33:A3091 1992. Unique Identifier : AIDSLINE ICDB/92685624
Schultz RJ; Bader JP; Chimirri A; Covey JM; Hill DL; Haugwitz RD; Guziec FS; Narayanan VL; Developmental Therapeutics Program, DCT, NCI, Bethesda, MD 20892

Abstract: The acquisition/screening programs of the NCI have identified thiazolobenzimidazoles as a novel class of anti-HIV agents. The most active member of this structural class, NSC 625487 (R = 2,6-di-F; structure shown in a diagram), protects T4 lymphocytes from the cytopathic effects of HIV-1 at levels of about 1 uM. The compound is effective in the p24 viral protein and infectious virus assays, and is also an inhibitor of HIV-1 reverse transcriptase. NSC 625487 is inactivated rapidly in vivo by metabolism to its sulfone and two isomeric sulfoxides. Synthetic efforts are underway to block the metabolism with retention of anti-HIV activity.

Keywords: Antiviral Agents/*PHARMACOLOGY Benzimidazoles/*PHARMACOLOGY Comparative Study Drug Design Human HIV/*DRUG EFFECTS HIV-1/*DRUG EFFECTS/ENZYMOLOGY Molecular Structure RNA-Directed DNA Polymerase/*ANTAGONISTS & INHIB T-Lymphocytes/DRUG EFFECTS Thiazoles/*PHARMACOLOGY ABSTRACT
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M92A1027

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