Design, synthesis, and SAR studies of novel and highly active tri-cyclic HIV integrase inhibitors

Bioorg Med Chem Lett. 2006 Aug 1;16(15):3989-92. doi: 10.1016/j.bmcl.2006.05.016. Epub 2006 May 24.

Abstract

A novel class of tri-cyclic HIV integrase inhibitors were designed based on conformational analysis of 1,6-naphthyridine carboxamide compound L-870810 and docking the designed inhibitor into the active site of our integrase enzyme model. The efficient syntheses of pyrroloquinoline tri-cyclic analogs are described. The SAR studies resulted in the identification of a lead compound that is more potent and more soluble than L-870810.

MeSH terms

  • Drug Design
  • HIV Integrase Inhibitors / chemical synthesis*
  • HIV Integrase Inhibitors / pharmacology*
  • Naphthyridines / chemistry
  • Structure-Activity Relationship

Substances

  • HIV Integrase Inhibitors
  • L870810
  • Naphthyridines