Rifamycins as inhibitors of retroviral reverse transcriptase from M-MuLV, RAV-2, and HIV-1

Farmaco. 1992 Nov;47(11):1367-83.

Abstract

29 Rifamycins were tested for inhibition of Reverse Transcriptase (RT) as potential anti HIV drugs. Two purified commercial enzymes from M-MuLV and RAV-2 were used. Anti-RT activity was also measured on a crude lysate of HIV-1. The results show that some derivatives have interesting levels of activity on isolated M-MuLV and RAV-2 RTs, while they are less active on the RT in the crude HIV-1 lysate. The active derivatives include oximes and hydrazones, alkylaminoderivatives, open ansa-chain derivatives and derivatives carrying a modified nucleoside.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • HIV Reverse Transcriptase
  • HIV-1 / enzymology
  • Leukemia Virus, Murine / enzymology
  • Molecular Weight
  • Retroviridae / enzymology*
  • Reverse Transcriptase Inhibitors*
  • Rifamycins / chemical synthesis
  • Rifamycins / pharmacology*

Substances

  • Reverse Transcriptase Inhibitors
  • Rifamycins
  • HIV Reverse Transcriptase