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


Singh, P; Sachdeva, S; Raj, R; Kumar, V; Mahajan, MP; Nasser, S; Vivas, L; Gut, J; Rosenthal, PJ; Feng, TS; Chibale, K; (2011) Antiplasmodial and cytotoxicity evaluation of 3-functionalized 2-azetidinone derivatives. Bioorganic & medicinal chemistry letters, 21 (15). pp. 4561-4563. ISSN 0960-894X DOI: https://doi.org/10.1016/j.bmcl.2011.05.119

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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.

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
Faculty and Department: Faculty of Infectious and Tropical Diseases > Dept of Immunology and Infection
PubMed ID: 21705220
Web of Science ID: 292729900037
URI: http://researchonline.lshtm.ac.uk/id/eprint/268

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