Author(s): Kumar K, Pradines B, Madamet M, Amalvict R, Kumar V
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Abstract A series of ferrocenylchalcone-β-lactam conjugates were synthesized and evaluated against 3D7 (CQ-Sensitive) and W2 (CQ-Resistant) strains of Plasmodium falciparum. The SAR studies revealed the dependence of activities at N-1 substituent of β-lactam ring with compounds being more potent on resistant strain. The compound 9f and 9l with N-cyclohexyl substituent proved to be the most potent and non-cytotoxic among the series exhibiting IC50 values of 2.36 and 2.43 μM respectively, against W2 strain of P. falciparum. Copyright © 2014 Elsevier Masson SAS. All rights reserved.
This article was published in Eur J Med Chem
and referenced in Journal of Applied & Computational Mathematics