Antiplasmodial and cytotoxicity evaluation of 3-functionalized 2-azetidinone derivatives

Bioorg Med Chem Lett. 2011 Aug 1;21(15):4561-3. doi: 10.1016/j.bmcl.2011.05.119. Epub 2011 Jun 12.

Abstract

3-Azido-, 3-amino- and 3-(1,2,3-triazol-1-yl)-β-lactams were synthesized and evaluated for their antiplasmodial activity against four strains of Plasmodium falciparum and KB cells for their cytotoxicity profiles. The presence of a cyclohexyl substituent at N-1 and a phenyl group on the triazole ring markedly improved the activity profiles of triazole-tethered β-lactam exhibiting IC(50) values of 1.13, 1.21 and 1.00 μM against 3D7, K1 and W2 strains respectively.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antimalarials / chemical synthesis
  • Antimalarials / chemistry*
  • Antimalarials / toxicity
  • Azetidines / chemical synthesis
  • Azetidines / chemistry*
  • Azetidines / toxicity
  • Cell Line, Tumor
  • Humans
  • Plasmodium falciparum / drug effects
  • Triazoles / chemistry
  • beta-Lactams / chemistry

Substances

  • 2-azetidinone
  • Antimalarials
  • Azetidines
  • Triazoles
  • beta-Lactams