Synthesis and Activity of a New Series of Antileishmanial Agents
Synthesis and Activity of a New Series of Antileishmanial Agents
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DOI：
10.1021/acsmedchemlett.7b00039
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发表时间：
2017-08-01
影响因子：
4.2
通讯作者：
Leahy, James W.
中科院分区：
文献类型：
--
作者：
Kanwar, Ankush;Eduful, Benjamin J.;Leahy, James W.
我们已经确定，四氢吲唑类化合物如1对杜氏利什曼原虫（利什曼病的病原体）显示出有效的活性。虽然以前已经探索了1的Hsp90活性和抗癌性质，但我们在这里提出我们的努力来优化它们对L. donovani通过合成设计用于探测原生动物Hsp90直向同源物的疏水口袋的新型类似物，特别是通过嵌入支架中的胺的官能化的支持。
We have determined that tetrahydroindazoles such as 1 show potent activity against Leishmania donovani, the causative agent of leishmaniasis. While the Hsp90 activity and anticancer properties of 1 have previously been explored, we present here our efforts to optimize their activity against L. donovani via the synthesis of novel analogues designed to probe the hydrophobic pocket of the protozoan Hsp90 orthologue, specifically through the auspices of functionalization of an amine embedded into the scaffold.