alexa 1H-1,2,3-triazole tethered mono- and bis-ferrocenylchalcone-β-lactam conjugates: synthesis and antimalarial evaluation.


Journal of Applied & Computational Mathematics

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

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