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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