Quinoline, Coumarin and Other Heterocyclic Analogs Based HIV-1 Integrase Inhibitors

Curr Drug Discov Technol. 2018;15(1):2-19. doi: 10.2174/1570163814666170531115452.

Abstract

Human Immunodeficiency Virus Type 1 Integrase or HIV-1 integrase (IN) is a 288 amino acid protein that incorporates the retrotranscribed viral DNA into the host chromosomal DNA. Over the past 30 years, large number of derivatives have been evaluated for their inhibitory potential against IN. There is vast literature available which need to be collated to help scientists plan the future drug design. This review discusses the reports of past 25 years on analogs of quinoline, coumarin and other related heterocycles, which exhibit low micromolar inhibitory potency against IN.

Keywords: 3'-end processing inhibitors; HIV-1 integrase; coumarins; heterocyclic analogs; quinolines; strand transfer inhibitors.

Publication types

  • Review

MeSH terms

  • Coumarins* / pharmacology
  • Coumarins* / therapeutic use
  • HIV Infections / drug therapy
  • HIV Infections / metabolism
  • HIV Integrase / chemistry
  • HIV Integrase / metabolism*
  • Humans
  • Integrase Inhibitors* / pharmacology
  • Integrase Inhibitors* / therapeutic use
  • Quinolines* / pharmacology
  • Quinolines* / therapeutic use

Substances

  • Coumarins
  • Integrase Inhibitors
  • Quinolines
  • HIV Integrase
  • p31 integrase protein, Human immunodeficiency virus 1