Thiourea-functionalized aminoglutethimide derivatives as anti-leishmanial agents.

Future Med Chem

H.E.J. Research Institute of Chemistry, International Center for Chemical & Biological Sciences, University of Karachi, Karachi, 75270, Pakistan.

Published: August 2024

We aim to develop new anti-leishmanial agents against and . A total of 23 thiourea derivatives of (±)-aminoglutethimide were synthesized and evaluated for activity against promastigotes of and . The -benzoyl analogue was found potent (IC = 12.7 μM) against and non toxic to normal cells. The docking studies, indicates that these inhibitors may target folate and glycolytic pathways of the parasite. The -hexyl compound was found strongly active against both species, and lacked cytotoxicity against normal cells, whereas compound , with a 3,5-bis-(tri-fluoro-methyl)phenyl unit, was active against , but was cytotoxic in nature. Compound was thus identified as a hit for further studies.

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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC11370960PMC
http://dx.doi.org/10.1080/17568919.2024.2359362DOI Listing

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