氮杂乙烯砜类化合物的合成及其作为抗疟药物的评价。
Aza vinyl sulfones: synthesis and evaluation as antiplasmodial agents.
机构信息
Research Institute for Medicines and Pharmaceutical Sciences (iMed.UL), Faculty of Pharmacy, University of Lisbon, Av. Prof. Gama Pinto, 1649-003 Lisbon, Portugal.
出版信息
Bioorg Med Chem. 2011 Dec 15;19(24):7635-42. doi: 10.1016/j.bmc.2011.10.018. Epub 2011 Oct 14.
A series of novel aza vinyl sulfones were designed, synthesized in good yields and evaluated as antiplasmodial agents. Tested compounds did not show activity against papain or the Plasmodium falciparum cysteine protease falcipain-2. However, a number of the new compounds effectively inhibited the in vitro development of P. falciparum. Compounds containing a squaramide group were the most active, with IC(50) values between 0.95 and 4.5 μM, suggesting that these are potential lead compounds for the development of new antimalarial agents.
我们设计、合成了一系列新型的氮杂乙烯砜类化合物，并评估了它们作为抗疟原虫药物的活性。测试的化合物对木瓜蛋白酶或恶性疟原虫半胱氨酸蛋白酶 falcipain-2 没有活性。然而，许多新化合物能有效地抑制恶性疟原虫的体外发育。含有酰亚胺基的化合物最为活跃，IC50 值在 0.95 到 4.5 μM 之间，这表明它们是开发新型抗疟药物的潜在先导化合物。
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