1H-1,2,3-triazole tethered isatin-ferrocene conjugates: Synthesis and in vitro antimalarial evaluation

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

来源：European Journal of Medicinal Chemistry, 2014, 87: 801-804.

DOI：10.1016/j.ejmech.2014.10.024

• Isatin-ferrocene conjugates
• Click chemistry
• Structure activity relationship
• Antimalarial evaluation
• Cytotoxicity

1H-1,2,3-triazole tethered isatin-ferrocene conjugates were synthesized and evaluated for their anti-plasmodial activities against chloroquine-susceptible (3D7) and chloroquine-resistant (W2) strains of Plasmodium falciparum. The conjugates 5f and 5h with an optimum combination of electron-withdrawing halogen substituent at C-5 position of isatin ring and a propyl chain, introduced as linker, proved to be most potent and non-cytotoxic among the series with IC50 values of 3.76 and 4.58 mu M against 3D7 and W2 strains, respectively.

• 出版日期2014-11-24