Synthesis and evaluation of quinoxalinones as HIV-1 reverse transcriptase inhibitors

Bioorg Med Chem Lett. 2000 Aug 7;10(15):1729-31. doi: 10.1016/s0960-894x(00)00321-8.

Abstract

A series of 3,3-disubstituted quinoxalinones was prepared and evaluated as HIV-1 reverse transcriptase inhibitors. The N-allyl (6b and 6f), N-cyclopropylmethyl (6a, 6g, 6h, and 6k) and N-carboalkoxy (6m-6y) substituted compounds displayed activity comparable or better than Efavirenz and GW420867X.

MeSH terms

  • Drug Evaluation
  • HIV Reverse Transcriptase / drug effects*
  • Quinoxalines / chemical synthesis*
  • Quinoxalines / pharmacology*
  • Reverse Transcriptase Inhibitors / chemical synthesis*
  • Reverse Transcriptase Inhibitors / pharmacology*

Substances

  • Quinoxalines
  • Reverse Transcriptase Inhibitors
  • HIV Reverse Transcriptase