Thiourea-functionalized aminoglutethimide derivatives as anti-Leishmanial agents

Muhammad Sajid, Hina Siddiqui, Humaira Zafar, Sammer Yousuf, Michael Threadgill, Muhammad I. Choudhary

Research output: Contribution to journalArticlepeer-review


Aims: We aimed to develop new anti-leishmanial agents against Leishmania major and Leishmania tropica. Materials & Methods: Twenty three 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 to be strongly active against both species and lacked cytotoxicity against normal cells, whereas compound 7r, with a 3,5-bis-(trifluoromethyl)phenyl unit, was active against Leishmania but was cytotoxic in nature. Compound 7v was thus identified as a hit for further studies.
Original languageEnglish
JournalFuture Medicinal Chemistry
Publication statusAcceptance date - 8 May 2024

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