Antiplasmodial and cytotoxicity evaluation of 3-functionalized 2-azetidinone derivatives.
Pardeep Singh;
Shaveta Sachdeva;
Raghu Raj;
Vipan Kumar;
Mohinder P Mahajan;
Shereen Nasser;
Livia Vivas;
Jiri Gut;
Phillip J Rosenthal;
Tzu-Shean Feng;
+1 more...
Kelly Chibale;
(2011)
Antiplasmodial and cytotoxicity evaluation of 3-functionalized 2-azetidinone derivatives.
Bioorganic & medicinal chemistry letters, 21 (15).
pp. 4561-4563.
ISSN 0960-894X
DOI: 10.1016/j.bmcl.2011.05.119
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.
| Item Type | Article |
|---|---|
| Keywords | c-3 Functionalized b-lactams, Triazoles, Click chemistry, Antiplasmodial, evaluation, lactam synthon method, building-blocks, beta-lactams, asymmetric-synthesis, malaria, podophyllotoxins, lankacidins, resistance, drug |
| ISI | 292729900037 |