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.
Pardeep Singh  1 ,  Shaveta Sachdeva ,  Raghu Raj ,  Vipan Kumar ,  Mohinder P Mahajan ,  Shereen Nasser ,  Livia Vivas ,  Jiri Gut ,  Phillip J Rosenthal ,  Tzu-Shean Feng ,  Kelly Chibale
Affiliations
  • 1. Department of Chemistry, Guru Nanak Dev University, Amritsar, India.
PMID: 21705220 DOI: 10.1016/j.bmcl.2011.05.119
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.