Synthesis of hydrazinyl-thiazole ester derivatives, in vitro trypanocidal and leishmanicidal activities.
Muhammad HaroonTashfeen AkhtarHasnain MehmoodAline C da Silva SantosJuliana M da ConceiçãoGraziella Leite BrondaniRobert da Silva TibúrcioPolicarpo Ademar Sales-JuniorValéria Rêgo Alves PereiraPublished in: Future medicinal chemistry (2024)
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.
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