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. 1995 Feb;39(2):539–541. doi: 10.1128/aac.39.2.539

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

G Piras 1, G E Dutschman 1, G J Im 1, B C Pan 1, S H Chu 1, Y C Cheng 1
PMCID: PMC162575  PMID: 7537030

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.

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Selected References

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