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. 2012 Aug 1;22(15):5046-50.
doi: 10.1016/j.bmcl.2012.06.010. Epub 2012 Jun 9.

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

Dennis S B Ongarora  1 , Jiri Gut, Philip J Rosenthal, Collen M Masimirembwa, Kelly Chibale
Affiliations

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

Dennis S B Ongarora et al. Bioorg Med Chem Lett. .

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 IC(50)s ranging from 7 to 22 nM.

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