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