Synthesis and biological evaluation of coumarin derivatives as inhibitors of Mycobacterium bovis (BCG)

Chem Biol Drug Des. 2012 Dec;80(6):929-36. doi: 10.1111/cbdd.12044.

Abstract

The coumarin compounds are an important class of biologically active molecules, which have attractive caught the attention of many organic and medicinal chemists, due to potential pharmaceutical implications and industrial applications. We herein report the one-pot procedure for the efficient synthesis of coumarin derivatives using commercially available substrates via isocyanide-based multicomponent condensation reactions. These compounds were evaluated for anti-mycobacterium activity against Mycobacterium bovis (Bacillus Calmette-Guerin). The preliminary results indicated that all of the tested compounds showed relatively good activity against the test organism. The compounds 7e, 7l, and 7m showed high anti-tuberculosis activity.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antitubercular Agents / chemical synthesis*
  • Antitubercular Agents / chemistry
  • Antitubercular Agents / pharmacology
  • Coumarins / chemical synthesis
  • Coumarins / chemistry*
  • Coumarins / pharmacology
  • Cyanides / chemistry
  • Microbial Sensitivity Tests
  • Mycobacterium bovis / drug effects*

Substances

  • Antitubercular Agents
  • Coumarins
  • Cyanides
  • coumarin