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

摘要

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. (c) 2014 Elsevier Masson SAS. All rights reserved.