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Synthesis of hydrazinyl-thiazole ester derivatives, in vitro trypanocidal and leishmanicidal activities.

Authors :
Haroon M
Akhtar T
Mehmood H
da Silva Santos AC
da Conceição JM
Brondani GL
Silva Tibúrcio RD
Galindo Bedor DC
Viturino da Silva JW
Sales Junior PA
Alves Pereira VR
Lima Leite AC
Source :
Future medicinal chemistry [Future Med Chem] 2024 Feb; Vol. 16 (3), pp. 221-238. Date of Electronic Publication: 2024 Jan 25.
Publication Year :
2024

Abstract

Aim: To synthesize novel more potent trypanocidal and leishmanicidal agents. Methods: Hantzsch's synthetic strategy was used to synthesize 1,3-thiazole-4-carboxylates and their N -benzylated derivatives. Results: 28 new thiazole-carboxylates and their N -benzylated derivatives were established to test their trypanocidal and leishmanicidal activities. From both series, compounds 3b , 4f , 4g , 4j and 4n exhibited a better or comparable trypanocidal profile to benznidazole. Among all tested compounds, 4n was found to be the most potent and was better than benznidazole. Conclusion: Further variation of substituents around 1,3-thiazole-4-carboxylates and or hydrazinyl moiety may assist in establishing better and more potent trypanocidal and leishmanicidal agents.

Details

Language :
English
ISSN :
1756-8927
Volume :
16
Issue :
3
Database :
MEDLINE
Journal :
Future medicinal chemistry
Publication Type :
Academic Journal
Accession number :
38269432
Full Text :
https://doi.org/10.4155/fmc-2023-0255