Action of uracil analogs on human immunodeficiency virus type 1 and its reverse transcriptase.

Antimicrobial Agents and Chemotherapy
G PirasY C Cheng

Abstract

Three structural analogs of 5-ethyl-1-benzyloxymethyl-6-(phenylthio)uracil (E-BPU) inhibited human immunodeficiency virus type 1 (HIV-1) replication without cytotoxicity in vitro and were more potent than azidothymidine and were as potent as E-BPU. The target of these compounds is HIV-1 reverse transcriptase. Reverse transcriptases resistant to nevirapine (tyrosine at position 181 to cysteine) and TIBO R82150 (leucine at position 100 to isoleucine) are cross resistant to E-BPU analogs. Nevirapine- or TIBO R82150-resistant HIV-1 were cross resistant to E-BPU analogs but were inhibited at concentrations 11- to 135-fold lower than the cytotoxic doses.

References

Mar 17, 1992·Biochemical Pharmacology·E Tramontano, Y C Cheng
Jan 1, 1990·Annals of the New York Academy of Sciences·Y C ChengM C Starnes
Aug 1, 1991·Proceedings of the National Academy of Sciences of the United States of America·M E GoldmanJ M Hoffman
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