Synthesis and evaluation of novel 6-(3,5-dimethylbenzyl)uracil analogs as potential anti-HIV-1 agents

Bioorg Khim. 2014 Sep-Oct;40(5):629-35. doi: 10.7868/s0132342314040058.

Abstract

A novel series of uracil derivatives with a 3,5-dimethylbenzyl group at the C-6 position were synthesized and evaluated as non-nucleoside HIV-1 reverse transcriptase inhibitors. Purity of the compounds has been confirmed by TLC. Structures of these compounds were established on the basis of elemental analyses and spectral studies. Some of the tested compounds showed moderate to potent activities against wild-type HIV-1, and N-1 alkylated derivatives were highly active.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-HIV Agents / administration & dosage
  • Anti-HIV Agents / chemical synthesis
  • Anti-HIV Agents / chemistry*
  • Cell Line
  • HIV Infections / drug therapy*
  • HIV Infections / virology
  • HIV Reverse Transcriptase / antagonists & inhibitors
  • HIV-1 / drug effects*
  • HIV-1 / enzymology
  • Humans
  • Structure-Activity Relationship
  • Uracil / analogs & derivatives
  • Uracil / chemical synthesis
  • Uracil / chemistry*

Substances

  • Anti-HIV Agents
  • Uracil
  • reverse transcriptase, Human immunodeficiency virus 1
  • HIV Reverse Transcriptase