Benzoheterocyclic amodiaquine analogues with potent antiplasmodial activity: Synthesis and pharmacological evaluation

…, PJ Rosenthal, CM Masimirembwa, K Chibale

Index: Ongarora, Dennis S.B.; Gut, Jiri; Rosenthal, Philip J.; Masimirembwa, Collen M.; Chibale, Kelly Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 15 p. 5046 - 5050

Full Text: HTML

Citation Number: 13

Abstract

The synthesis and evaluation of antiplasmodial activity of benzothiazole, benzimidazole, benzoxazole and pyridine analogues of amodiaquine is hereby reported. Benzothiazole and benzoxazole analogues with a protonatable tertiary nitrogen atom possessed excellent activity against the W2 and K1 chloroquine resistant strains of Plasmodium falciparum, with IC50s ranging from 7 to 22nM.