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Synthesis and Activity of a New Series of Antileishmanial Agents
ACS Medicinal Chemistry Letters ( IF 4.2 ) Pub Date : 2017-08-02 00:00:00 , DOI: 10.1021/acsmedchemlett.7b00039
Ankush Kanwar 1 , Benjamin J Eduful 1 , Linda Barbeto 1 , Piero Carletti Bonomo 1 , Andrea Lemus 1 , Brian A Vesely 2 , Tina S Mutka 2 , Ala Azhari 2 , Dennis E Kyle 2 , James W Leahy 1, 3, 4
Affiliation  

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.

中文翻译:

新型抗利什曼药剂的合成及活性

我们已确定四氢吲唑如1对利什曼病的病原体Leishmania donovani显示出有效的活性。虽然之前已经探索了1的 Hsp90 活性和抗癌特性,但我们在这里展示了我们通过合成新的类似物来优化它们对L. donovani的活性,这些类似物旨在探测原生动物 Hsp90 直系同源物的疏水口袋,特别是通过嵌入支架中的胺的功能化。
更新日期:2017-08-02
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