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. 2014 Oct 30:86:113-21.
doi: 10.1016/j.ejmech.2014.08.053. Epub 2014 Aug 16.

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

Kewal Kumar  1 , Bruno Pradines  2 , Marilyn Madamet  3 , Rémy Amalvict  3 , Vipan Kumar  4
Affiliations

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

Kewal Kumar et al. Eur J Med Chem. .

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.

Keywords: 1H-1,2,3-triazoles; Click chemistry; Ferrcenylchalcone-β-lactam conjugates; Plasmodium falciparum; Structure–activity relationship.

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