Synthesis and Activity of a New Series of Antileishmanial Agents

Authors

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

Document Type

Article

Publication Date

2017

Digital Object Identifier (DOI)

https://doi.org/10.1021/acsmedchemlett.7b00039

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.

Was this content written or created while at USF?

Yes

Citation / Publisher Attribution

ACS Medicinal Chemistry Letters, v. 8, issue 8, p. 797-801

Scholar Commons Citation

Kanwar, Ankush; Eduful, Benjamin J.; Barbeto, Linda; Bonomo, Piero Carletti; Lemus, Andrea; Vesely, Brian A.; Mutka, Tina S.; Azhari, Ala; Kyle, Dennis E.; and Leahy, James W., "Synthesis and Activity of a New Series of Antileishmanial Agents" (2017). Chemistry Faculty Publications. 183.
https://digitalcommons.usf.edu/chm_facpub/183