Substituted indoles as HIV-1 non-nucleoside reverse transcriptase inhibitors: a patent evaluation (WO2015044928)

Expert Opin Ther Pat. 2016 May;26(5):629-35. doi: 10.1517/13543776.2016.1135902. Epub 2016 Feb 16.

Abstract

The invention described in this patent (WO2015044928) is related to compounds based on the substituted indole scaffold, their synthetic process and application to inhibit HIV-1 replication as non-nucleoside reverse transcriptase inhibitors (NNRTIs). Some of the newly claimed compounds presented improved potency against wild-type (WT) HIV-1 strain in comparison to previously disclosed indole-based NNRTIs and were also shown to be effective against common resistant HIV-1 strains. In light of their novel structural characteristics, simple synthetic route and improved anti-HIV activity, these compounds deserve further study as promising NNRTIs.

Keywords: HIV; antiviral activity; heterocycle; non-nucleoside reverse transcriptase inhibitors; substituted indole.

MeSH terms

  • Anti-HIV Agents / chemistry
  • Anti-HIV Agents / pharmacology*
  • Drug Design
  • Drug Resistance, Viral
  • HIV Infections / drug therapy*
  • HIV Infections / enzymology
  • HIV Reverse Transcriptase / antagonists & inhibitors
  • Humans
  • Indoles / chemistry
  • Indoles / pharmacology*
  • Patents as Topic
  • Reverse Transcriptase Inhibitors / chemistry
  • Reverse Transcriptase Inhibitors / pharmacology*

Substances

  • Anti-HIV Agents
  • Indoles
  • Reverse Transcriptase Inhibitors
  • reverse transcriptase, Human immunodeficiency virus 1
  • HIV Reverse Transcriptase