通过天然产物共轭合成一种有效的抗疟药物。
Synthesis of a potent antimalarial agent through natural products conjugation.
机构信息
Dipartimento di Chimica, Università degli Studi di Milano, Via C. Golgi 19, 20133 Milano, Italy.
出版信息
ChemMedChem. 2013 Feb;8(2):221-5. doi: 10.1002/cmdc.201200503. Epub 2013 Jan 10.
Abstract
Au naturel! (+)-Usnic acid (green) is a weak antimalarial agent, however, in conjugation with known antimalarial scaffolds and drugs, such as dihydroartemisinin (blue), potent activity against the blood-stage parasite can be seen both in vitro and in vivo. The compound shown exhibits an IC(50) value of 1.4 nM against Plasmodium falciparum in vitro and proved nearly as efficacious as artesunate in a mouse model of infection.
摘要
纯天然！（+）-地衣酸（绿色）是一种弱抗疟药物，然而，与已知的抗疟支架和药物（如双氢青蒿素（蓝色））结合使用，在体外和体内都可以看到对血阶段寄生虫的有效活性。所示化合物对体外疟原虫的 IC50 值为 1.4 nM，在感染的小鼠模型中证明与青蒿琥酯几乎同样有效。
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