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Elsevier, Bioorganic and Medicinal Chemistry Letters, 15(21), p. 4561-4563
DOI: 10.1016/j.bmcl.2011.05.119
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Antiplasmodial and cytotoxicity evaluation of 3-functionalized 2-azetidinone derivatives
,
Mohinder P. Mahajan,
Shereen Nasser,
Livia Vivas,
Jiri Gut,
Pj Rosenthal,
Ts Feng,
Kelly Chibale
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Abstract
3-Azido-, 3-amino- and 3-(1,2,3-triazol-1-yl)-beta-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 beta-lactam exhibiting IC(50) values of 1.13, 1.21 and 1.00 mu M against 3D7, K1 and W2 strains respectively. (C) 2011 Elsevier Ltd. All rights reserved.