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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.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Singh P,Sachdeva S,Raj R,Kumar V,Mahajan MP,Nasser S,Vivas L,Gut J,Rosenthal PJ,Feng TS,Chibale K

doi

10.1016/j.bmcl.2011.05.119

subject

Has Abstract

pub_date

2011-08-01 00:00:00

pages

4561-3

issue

15

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(11)00760-8

journal_volume

21

pub_type

杂志文章

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