Synthesis and anti-HIV-1 activity of new delavirdine analogues carrying arylpyrrole moieties

Chem Pharm Bull (Tokyo). 2001 Nov;49(11):1406-11. doi: 10.1248/cpb.49.1406.

Abstract

In our search for novel anti-human immunodeficiency virus (HIV)-1 agents, 14 delavirdine analogues were synthesized and evaluated as potential anti-HIV-1 agents in cell-based assays. Compound 1Aa exhibited potent and selective anti-HIV-1 activity in acutely infected MT4 cells, with effective concentration (EC50) values in the submicromolar range.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-HIV Agents / chemical synthesis*
  • Anti-HIV Agents / pharmacology*
  • Cell Line
  • Delavirdine / analogs & derivatives*
  • Delavirdine / chemical synthesis*
  • Delavirdine / pharmacology*
  • Drug Evaluation, Preclinical / methods
  • Drug Evaluation, Preclinical / statistics & numerical data
  • HIV-1 / drug effects*
  • Humans

Substances

  • Anti-HIV Agents
  • Delavirdine