Synthesis of hydrazinyl–thiazole ester derivatives, <i>in vitro</i> trypanocidal and leishmanicidal activities-Reference-Cited by-同舟云学术

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

Published:2024-02 Issue:3 Volume:16 Page:221-238
ISSN:1756-8919
Container-title:Future Medicinal Chemistry
language:en
Short-container-title:Future Medicinal Chemistry

Author:

Haroon Muhammad¹^ORCID,Akhtar Tashfeen²^ORCID,Mehmood Hasnain²^ORCID,da Silva Santos Aline C³,da Conceição Juliana M⁴^ORCID,Brondani Graziella Leite⁴^ORCID,Silva Tibúrcio Robert da⁴^ORCID,Galindo Bedor Danilo C⁴^ORCID,Viturino da Silva José W⁴^ORCID,Sales Junior Policarpo A³^ORCID,Alves Pereira Valeria R³^ORCID,Lima Leite Ana C⁴^ORCID

Affiliation:

1. Department of Chemistry & Biochemistry, Miami University, 651 E High Street, Oxford, OH 45056, USA

2. Department of Chemistry, Mirpur University of Science & Technology (MUST), 10250-Mirpur (AJK), Pakistan

3. Aggeu Magalhães Institute, Fundação Oswaldo Cruz, 50670-420, Recife, PE, Brazil

4. Department of Pharmaceutical Sciences, Health Sciences Centre, Federal University of Pernambuco, 50740-520, Recife, PE, Brazil

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.

Publisher

Future Science Ltd

Subject

Drug Discovery,Pharmacology,Molecular Medicine

Link

https://www.future-science.com/doi/pdf/10.4155/fmc-2023-0255

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