二氢月桂酸脱氢酶
恶性疟原虫
化学
寄生虫寄主
疟疾
酶
EC50型
生物化学
药理学
酶抑制剂
体外
生物
免疫学
计算机科学
万维网
作者
Margaret A. Phillips,Ramesh Gujjar,Nicholas A. Malmquist,John White,Farah El Mazouni,Jeffrey Baldwin,Pradipsinh K. Rathod
摘要
A Plasmodium falciparum dihydroorotate dehydrogenase (PfDHODH) inhibitor that is potent (KI = 15 nM) and species-selective (>5000-fold over the human enzyme) was identified by high-throughput screening. The substituted triazolopyrimidine and its structural analogues were produced by an inexpensive three-step synthesis, and the series showed good association between PfDHODH inhibition and parasite toxicity. This study has identified the first nanomolar PfDHODH inhibitor with potent antimalarial activity in whole cells (EC50 = 79 nM).
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