Quantitative structure--activity correlations of rifamycins as inhibitors of viral RNA-directed DNA polymerase and mammalian alpha and beta DNA polymerases.

Important note: Information in this article was accurate in 1980. The state of the art may have changed since the publication date.

Quantitative structure--activity correlations of rifamycins as inhibitors of viral RNA-directed DNA polymerase and mammalian alpha and beta DNA polymerases.

J Med Chem. 1980 Mar;23(3):256-61. Unique Identifier : AIDSLINE MED/80162686
Wu RS; Wolpert-DeFilippes MK; Quinn FR

Abstract: Twenty-two 3-substituted rifamycins were tested for inhibition of mammalian alpha and beta DNA polymerase and viral RNA-dependent DNA polymerase (reverse transcriptase). Quantitative structure--activity relationships (QSAR) were formulated for the three systems. Inhibition is linearly dependent on the partition coefficient and is highly favored by the presence of bulky hydrazones or oximes. None of these agents proved to be a selective or specific inhibitor of reverse transcriptase. A correlation in terms of log P and (log P)2 was obtained from data on a more closely related set of analogues from a published study. For murine reverse transcriptase, log P0 = 5.1.

Keywords: Animal DNA Polymerases/*ANTAGONISTS & INHIB In Vitro Mathematics Mice Reverse Transcriptase/*ANTAGONISTS & INHIB Rifamycins/*PHARMACOLOGY Sarcoma Viruses, Simian/DRUG EFFECTS/ENZYMOLOGY Solubility Structure-Activity Relationship Support, U.S. Gov't, P.H.S. Viruses/*DRUG EFFECTS/ENZYMOLOGY JOURNAL ARTICLE

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