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

作者：Kumar Kewal; Pradines Bruno; Madamet Marilyn; Amalvict Remy; Kumar Vipan^*

来源：European Journal of Medicinal Chemistry, 2014, 86: 113-121.

DOI：10.1016/j.ejmech.2014.08.053

• Click chemistry
• Ferrcenylchalcone-beta-lactam conjugates
• 1H-1,2,3-triazoles
• Structure-activity relationship
• Plasmodium falciparum

A series of ferrocenylchalcone-beta-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 beta-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 mu M respectively, against W2 strain of P. falciparum.

• 出版日期2014-10-30