哒嗪并[1,2-a]嘧啶-4-酮类作为抗疟原虫 falcipain-2 抑制剂。
Pyrido[1,2-a]pyrimidin-4-ones as antiplasmodial falcipain-2 inhibitors.
机构信息
Pharmacy Department, Faculty of Tech. and Engg., The M S University of Baroda, Vadodara 390 001,Gujarat, India.
出版信息
Bioorg Med Chem. 2012 Nov 1;20(21):6296-304. doi: 10.1016/j.bmc.2012.09.008. Epub 2012 Sep 13.
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.
恶性疟原虫半胱氨酸蛋白酶 falcipain-2（FP-2）是抗疟化疗的一个有前途的靶点，抑制这种蛋白酶会对寄生虫的生长产生不利影响。合成了一系列吡啶并[1,2-a]嘧啶-4-酮，并评估了它们对体外 FP-2 的抑制潜力。化合物（14,17）对 FP-2 具有优异的抑制作用，可作为进一步开发强效 FP-2 抑制剂作为潜在抗疟药物的先导化合物。
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