Literature DB >> 21705220

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

Pardeep Singh1, Shaveta Sachdeva, Raghu Raj, Vipan Kumar, Mohinder P Mahajan, Shereen Nasser, Livia Vivas, Jiri Gut, Phillip J Rosenthal, Tzu-Shean Feng, Kelly Chibale.   

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.
Copyright © 2011 Elsevier Ltd. All rights reserved.

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Year:  2011        PMID: 21705220     DOI: 10.1016/j.bmcl.2011.05.119

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  2 in total

1.  Molecular Diversity by Olefin Cross-Metathesis on Solid Support. Generation of Libraries of Biologically Promising β-Lactam Derivatives.

Authors:  Luciana Méndez; Andrés A Poeylaut-Palena; Ernesto G Mata
Journal:  Molecules       Date:  2018-05-16       Impact factor: 4.411

2.  Coupling the Antimalarial Cell Penetrating Peptide TP10 to Classical Antimalarial Drugs Primaquine and Chloroquine Produces Strongly Hemolytic Conjugates.

Authors:  Luísa Aguiar; Arnau Biosca; Elena Lantero; Jiri Gut; Nuno Vale; Philip J Rosenthal; Fátima Nogueira; David Andreu; Xavier Fernàndez-Busquets; Paula Gomes
Journal:  Molecules       Date:  2019-12-12       Impact factor: 4.411

  2 in total

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