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

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.