Synthesis of hydrazinyl-thiazole ester derivatives, in vitro trypanocidal and leishmanicidal activities
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.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2024 |
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| Erschienen: |
2024 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:16 |
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| Enthalten in: |
Future medicinal chemistry - 16(2024), 3 vom: 24. Jan., Seite 221-238 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Haroon, Muhammad [VerfasserIn] |
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| Links: |
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| Themen: |
1,3-thiazole-4-carboxylates |
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| Anmerkungen: |
Date Completed 30.01.2024 Date Revised 30.01.2024 published: Print-Electronic Citation Status MEDLINE |
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| doi: |
10.4155/fmc-2023-0255 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| PPN (Katalog-ID): |
NLM367598604 |
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| 520 | |a 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 | ||
| 650 | 4 | |a Journal Article | |
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| 700 | 1 | |a da Silva Santos, Aline C |e verfasserin |4 aut | |
| 700 | 1 | |a da Conceição, Juliana M |e verfasserin |4 aut | |
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| 700 | 1 | |a Silva Tibúrcio, Robert da |e verfasserin |4 aut | |
| 700 | 1 | |a Galindo Bedor, Danilo C |e verfasserin |4 aut | |
| 700 | 1 | |a Viturino da Silva, José W |e verfasserin |4 aut | |
| 700 | 1 | |a Sales Junior, Policarpo A |e verfasserin |4 aut | |
| 700 | 1 | |a Alves Pereira, Valeria R |e verfasserin |4 aut | |
| 700 | 1 | |a Lima Leite, Ana C |e verfasserin |4 aut | |
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