Synthesis, antimalarial and antitubercular activity of acetylenic chalcones

Bioorg Med Chem Lett. 2010 Feb 1;20(3):942-4. doi: 10.1016/j.bmcl.2009.12.062. Epub 2009 Dec 23.

Abstract

A series of acetylenic chalcones were evaluated for antimalarial and antitubercular activity. The antimalarial data for this series suggests that growth inhibition of the W2 strain of Plasmodium falciparum can be imparted by the introduction of a methoxy group ortho to the acetylenic group. Most compounds were more active against non-replicating than replicating cultures of Mycobacterium tuberculosis H(37)Rv, an unusual pattern with respect to existing anti-TB agents.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alkynes / chemical synthesis*
  • Alkynes / pharmacology
  • Antimalarials / chemical synthesis*
  • Antimalarials / pharmacology
  • Antitubercular Agents / chemical synthesis*
  • Antitubercular Agents / pharmacology
  • Chalcones / chemical synthesis*
  • Chalcones / pharmacology
  • Mycobacterium tuberculosis / drug effects
  • Mycobacterium tuberculosis / physiology
  • Plasmodium falciparum / drug effects
  • Plasmodium falciparum / physiology

Substances

  • Alkynes
  • Antimalarials
  • Antitubercular Agents
  • Chalcones