Pyrido [1, 2-a] pyrimidin-4-ones as antiplasmodial falcipain-2 inhibitors

…, J Huang, RC Gupta, SS Nadkarni, R Giridhar…

Index: Mane; Li; Huang; Gupta; Nadkarni; Giridhar; Naik; Yadav Bioorganic and Medicinal Chemistry, 2012 , vol. 20, # 21 p. 6296 - 6304

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Citation Number: 14

Abstract

Plasmodium falciparum cysteine protease falcipain-2 (FP-2) is a promising target for antimalarial chemotherapy and inhibition of this protease affects the growth of parasite adversely. A series of pyrido [1, 2-a] pyrimidin-4-ones were synthesized and evaluated for their in vitro FP-2 inhibitory potential. Compounds (14, 17) showed excellent FP-2 inhibition and can serve as lead compounds for further development of potent FP-2 inhibitors as ...