Thiourea-functionalized aminoglutethimide derivatives as anti-leishmanial agents.
Future Med Chem
; 16(15): 1485-1497, 2024 Aug 02.
Article
em En
| MEDLINE
| ID: mdl-38953461
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-methyl)phenyl unit, was active against Leishmania, but was cytotoxic in nature. Compound 7v was thus identified as a hit for further studies.
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Palavras-chave
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Tioureia
/
Leishmania tropica
/
Leishmania major
/
Antiprotozoários
Limite:
Animals
/
Humans
Idioma:
En
Revista:
Future Med Chem
Ano de publicação:
2024
Tipo de documento:
Article
País de afiliação:
Paquistão