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Synthesis and Activity of a New Series of Antileishmanial Agents.

ABSTRACT: 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.

SUBMITTER: Kanwar A 

PROVIDER: S-EPMC5554902 | biostudies-other | 2017 Aug

REPOSITORIES: biostudies-other

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Synthesis and Activity of a New Series of Antileishmanial Agents.

Kanwar Ankush A   Eduful Benjamin J BJ   Barbeto Linda L   Carletti Bonomo Piero P   Lemus Andrea A   Vesely Brian A BA   Mutka Tina S TS   Azhari Ala A   Kyle Dennis E DE   Leahy James W JW  

ACS medicinal chemistry letters 20170731 8

We have determined that tetrahydroindazoles such as <b>1</b> show potent activity against <i>Leishmania donovani</i>, the causative agent of leishmaniasis. While the Hsp90 activity and anticancer properties of <b>1</b> have previously been explored, we present here our efforts to optimize their activity against <i>L. donovani</i> via the synthesis of novel analogues designed to probe the hydrophobic pocket of the protozoan Hsp90 orthologue, specifically through the auspices of functionalization  ...[more]

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