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

被引：25
|
作者：
Mane, U. R. [1 ,2 ]
Li, H. [3 ]
Huang, J. [3 ]
Gupta, R. C. [2 ]
Nadkarni, S. S. [2 ]
Giridhar, R. [1 ]
Naik, P. P. [1 ]
Yadav, M. R. [1 ]
机构：
[1] Maharaja Sayajirao Univ Baroda, Dept Pharm, Fac Tech & Engg, Vadodara 390001, Gujarat, India
[2] Torrent Res Ctr, Village Bhat 382421, Gujarat, India
[3] E China Univ Sci & Technol, Shanghai 200237, Peoples R China
来源：
BIOORGANIC & MEDICINAL CHEMISTRY | 2012年 / 20卷 / 21期
关键词：
Pyrido[1,2-a]pyrimidin-4-one; Cysteine protease; Falcipain-2; inhibitor; Malaria; ANTIMALARIAL ACTIVITY; CYSTEINE PROTEASE; MALARIA;
D O I：
10.1016/j.bmc.2012.09.008
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
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 potential antimalarial drugs. (C) 2012 Elsevier Ltd. All rights reserved.
引用
收藏
页码：6296 / 6304
页数：9
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