Synthesis and evaluation of 2-pyridyl pyrimidines with in vitro antiplasmodial and antileishmanial activity
作者:Chitalu C. Musonda、Gavin A. Whitlock、Michael J. Witty、Reto Brun、Marcel Kaiser
DOI:10.1016/j.bmcl.2008.11.098
日期:2009.1
A series of 2-pyridyl pyrimidines, reported inhibitors of Plasmodium falciparum methionine aminopeptidase 1b were synthesized and evaluated for their antiplasmodial activities. An analysis of physicochemical properties demonstrated a link between lipophilicity and antiparasitic activity. Cross screening of the library against cultured Leishmania donovani parasites revealed this class of compounds as
合成了一系列2-吡啶基嘧啶,已报道恶性疟原虫蛋氨酸氨基肽酶1b的抑制剂,并评估了它们的抗血浆活性。理化性质的分析表明亲脂性和抗寄生虫活性之间的联系。针对培养的利什曼原虫donovani寄生虫的文库的交叉筛选揭示了这类化合物是体外寄生虫发展的有效抑制剂。