دورية أكاديمية
Synthesis of hydrazinyl-thiazole ester derivatives, in vitro trypanocidal and leishmanicidal activities.
| العنوان: | Synthesis of hydrazinyl-thiazole ester derivatives, in vitro trypanocidal and leishmanicidal activities. |
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| المؤلفون: | Haroon M; Department of Chemistry & Biochemistry, Miami University, 651 E High Street, Oxford, OH 45056, USA., Akhtar T; Department of Chemistry, Mirpur University of Science & Technology (MUST), 10250-Mirpur (AJK), Pakistan., Mehmood H; Department of Chemistry, Mirpur University of Science & Technology (MUST), 10250-Mirpur (AJK), Pakistan., da Silva Santos AC; Aggeu Magalhães Institute, Fundação Oswaldo Cruz, 50670-420, Recife, PE, Brazil., da Conceição JM; Department of Pharmaceutical Sciences, Health Sciences Centre, Federal University of Pernambuco, 50740-520, Recife, PE, Brazil., Brondani GL; Department of Pharmaceutical Sciences, Health Sciences Centre, Federal University of Pernambuco, 50740-520, Recife, PE, Brazil., Silva Tibúrcio RD; Department of Pharmaceutical Sciences, Health Sciences Centre, Federal University of Pernambuco, 50740-520, Recife, PE, Brazil., Galindo Bedor DC; Department of Pharmaceutical Sciences, Health Sciences Centre, Federal University of Pernambuco, 50740-520, Recife, PE, Brazil., Viturino da Silva JW; Department of Pharmaceutical Sciences, Health Sciences Centre, Federal University of Pernambuco, 50740-520, Recife, PE, Brazil., Sales Junior PA; Aggeu Magalhães Institute, Fundação Oswaldo Cruz, 50670-420, Recife, PE, Brazil., Alves Pereira VR; Aggeu Magalhães Institute, Fundação Oswaldo Cruz, 50670-420, Recife, PE, Brazil., Lima Leite AC; Department of Pharmaceutical Sciences, Health Sciences Centre, Federal University of Pernambuco, 50740-520, Recife, PE, Brazil. |
| المصدر: | Future medicinal chemistry [Future Med Chem] 2024 Feb; Vol. 16 (3), pp. 221-238. Date of Electronic Publication: 2024 Jan 25. |
| نوع المنشور: | Journal Article; Research Support, Non-U.S. Gov't |
| اللغة: | English |
| بيانات الدورية: | Publisher: Future Science Country of Publication: England NLM ID: 101511162 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1756-8927 (Electronic) Linking ISSN: 17568919 NLM ISO Abbreviation: Future Med Chem Subsets: MEDLINE |
| أسماء مطبوعة: | Original Publication: London : Future Science, 2009- |
| مواضيع طبية MeSH: | Trypanosoma cruzi* , Nitroimidazoles* , Trypanocidal Agents*/pharmacology, Thiazoles/pharmacology ; Esters/pharmacology |
| مستخلص: | 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. |
| فهرسة مساهمة: | Keywords: 1,3-thiazole-4-carboxylates; Trypanosoma cruzi; leishmaniasis; neglected tropical diseases Local Abstract: [plain-language-summary] Chagas disease and leishmaniasis are neglected tropical diseases. Herein, 28 1,3-thiazoles have been synthesized from thiosemicarbazones in a rapid, efficient and cost-effective manner. In vitro assays were performed against intracellular amastigotes of Trypanosoma cruzi ( T. cruzi ) and promastigotes and intracellular amastigote forms of Leishmania infantum ( L. infantum ) and Leishmania amazonensis ( L. amazonensis ). Some of the 1,3-thiazole-4-carboxylates inhibited the amastigote form of T. cruzi without affecting macrophage viability, compound 4n being the most potent and better than benznidazole. Our synthesized compounds exhibited promising activity against T. cruzi , thus broadening options for scaffold and lead compound optimization. Concerning the leishmanicidal activity, compound 4g was the best prototype in terms of potency and selectivity. Compounds 4g and 3m showed moderate selectivity and potency against intracellular amastigotes of L. amazonensis and L. infantum , respectively. |
| المشرفين على المادة: | YC42NRJ1ZD (benzonidazole) 0 (Thiazoles) 0 (Esters) 0 (Nitroimidazoles) 0 (Trypanocidal Agents) |
| تواريخ الأحداث: | Date Created: 20240125 Date Completed: 20240130 Latest Revision: 20240519 |
| رمز التحديث: | 20240520 |
| DOI: | 10.4155/fmc-2023-0255 |
| PMID: | 38269432 |
| قاعدة البيانات: | MEDLINE |
PDF full text from Publisher | تدمد: | 1756-8927 |
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| DOI: | 10.4155/fmc-2023-0255 |