New HIV-1 replication inhibitors of the styryquinoline class bearing aroyl/acyl groups at the C-7 position: synthesis and biological activity

Bioorg Med Chem Lett. 2005 Sep 15;15(18):4019-22. doi: 10.1016/j.bmcl.2005.06.036.

Abstract

Novel variants of HIV-1 replication inhibitors of the styrylquinoline class harboring aroyl/acyl group at the C-7 position have been synthesized. In sharp contrast with styrylquinolines bearing a carboxylic acid group at C-7, these compounds proved to be inactive toward HIV-1 integrase in in vitro assays.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acylation
  • Anti-HIV Agents / chemical synthesis*
  • Anti-HIV Agents / chemistry
  • Anti-HIV Agents / pharmacology*
  • Anti-HIV Agents / toxicity
  • HIV Integrase / metabolism
  • HIV-1 / drug effects*
  • HIV-1 / physiology*
  • Inhibitory Concentration 50
  • Molecular Structure
  • Quinolines / chemical synthesis
  • Quinolines / chemistry*
  • Quinolines / pharmacology*
  • Quinolines / toxicity
  • Structure-Activity Relationship
  • Virus Replication / drug effects*

Substances

  • Anti-HIV Agents
  • Quinolines
  • HIV Integrase