Synthesis and Activity of a New Series of Antileishmanial Agents.

Ankush Kanwar, Benjamin J Eduful,Linda Barbeto, Piero Carletti Bonomo, Andrea Lemus,Brian A Vesely,Tina S Mutka,Ala Azhari,Dennis E Kyle,James W Leahy

ACS MEDICINAL CHEMISTRY LETTERS(2017)

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摘要
We have determined that tetrahydroindazoles such as show potent activity against , the causative agent of leishmaniasis. While the Hsp90 activity and anticancer properties of have previously been explored, we present here our efforts to optimize their activity against 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.
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关键词
Antiinfectives,Hsp90,chaperone,leishmaniasis
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