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Synthesis and Activity of a New Series of Antileishmanial Agents
ACS Medicinal Chemistry Letters ( IF 3.5 ) 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
ACS Medicinal Chemistry Letters ( IF 3.5 ) 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
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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：
一系列新的抗leishmanialant剂的合成和活性。
我们已经确定四氢吲哚类化合物（如1）显示出对利什曼原虫病的致病因子多氏利什曼原虫的有效活性。虽然以前已经研究过Hsp90的活性和1的抗癌特性，但在此我们通过合成旨在探测原生动物Hsp90直向同源物的疏水口袋的新类似物，特别是通过Hsp90的疏水性口袋，来优化其对donovani的活性。嵌入支架的胺的功能化。
更新日期：2017-08-02
中文翻译：
一系列新的抗leishmanialant剂的合成和活性。
我们已经确定四氢吲哚类化合物（如1）显示出对利什曼原虫病的致病因子多氏利什曼原虫的有效活性。虽然以前已经研究过Hsp90的活性和1的抗癌特性，但在此我们通过合成旨在探测原生动物Hsp90直向同源物的疏水口袋的新类似物，特别是通过Hsp90的疏水性口袋，来优化其对donovani的活性。嵌入支架的胺的功能化。
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