Thiourea-functionalized aminoglutethimide derivatives as anti-leishmanial agents.

ABSTRACT: Aim: We aim to develop new anti-leishmanial agents against Leishmania major and Leishmania tropica.Materials & methods: A total of 23 thiourea derivatives of (±)-aminoglutethimide were synthesized and evaluated for in vitro activity against promastigotes of L. major and L. tropica.Results & conclusion: The N-benzoyl analogue 7p was found potent (IC₅₀ = 12.7 μM) against L. major and non toxic to normal cells. The docking studies, indicates that these inhibitors may target folate and glycolytic pathways of the parasite. The N-hexyl compound 7v was found strongly active against both species, and lacked cytotoxicity against normal cells, whereas compound 7r, with a 3,5-bis-(tri-fluoro-m

SUBMITTER: Sajid M 

PROVIDER: S-EPMC11370960 | biostudies-literature | 2024 Aug

REPOSITORIES: biostudies-literature