Naphthoxazepine inhibitors of HIV-1 integrase: synthesis and biological evaluation

ChemMedChem. 2008 Jun;3(6):986-90. doi: 10.1002/cmdc.200800026.

Abstract

Two sets of compounds derived from the fusion of a diversely annulated naphthoxazepinedione system with 1,3-thiazole and 1,3-oxazole are described. These compounds are close analogues of previously reported thiazolothiazepine inhibitors of human immunodeficiency virus type 1 integrase (HIV-1 IN). Some of the new derivatives show potency similar to that of the reference compounds, thus gaining further insight into the structure-activity relationship of this class of IN inhibitors.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antiviral Agents / chemical synthesis
  • Antiviral Agents / chemistry
  • Antiviral Agents / pharmacology
  • Drug Design
  • HIV Integrase / drug effects*
  • HIV Integrase Inhibitors / chemical synthesis*
  • HIV Integrase Inhibitors / chemistry
  • HIV Integrase Inhibitors / pharmacology*
  • HIV-1 / drug effects*
  • Humans
  • Microbial Sensitivity Tests
  • Models, Molecular
  • Molecular Structure
  • Oxazepines / chemical synthesis*
  • Oxazepines / chemistry
  • Oxazepines / pharmacology*
  • Stereoisomerism
  • Structure-Activity Relationship

Substances

  • Antiviral Agents
  • HIV Integrase Inhibitors
  • Oxazepines
  • HIV Integrase
  • p31 integrase protein, Human immunodeficiency virus 1