Piperazine-1,2,3-triazole scaffolds : design, synthesis, anticancer and antimicrobial evaluation
Aim: The objective of the present study is to design and synthesize diverse piperazine-1,2,3-triazole scaffolds as key pharmacophores possessing antimicrobial/anticancer activities. Materials & methods: Twenty-four scaffolds were synthesized via a click-inspired synthetic protocol and were assayed for anticancer activity using the methyl thiazolyl tetrazolium assay and for antimicrobial potency by serial dilution. Results: Among all the tested 1,2,3-triazole scaffolds, compounds 7i (IC50: 5.22 ± 0.05 μM) and 7a (IC50: 5.34 ± 0.13 μM) exhibited good anticancer activity, and 7x also showed notable antimicrobial activity. Molecular docking studies of potent analogs 7i and 7a were performed to provide an insight into their binding interactions. Conclusion: Compound 7x is considered a valuable lead compound for further optimization of anticancer and antimicrobial agents.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2023 |
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| Erschienen: |
2023 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:15 |
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| Enthalten in: |
Future medicinal chemistry - 15(2023), 8 vom: 18. Apr., Seite 679-697 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Yadav, Priyanka [VerfasserIn] |
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| Links: |
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| Themen: |
1,2,3-triazole |
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| Anmerkungen: |
Date Completed 18.05.2023 Date Revised 25.05.2023 published: Print-Electronic Citation Status MEDLINE |
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| doi: |
10.4155/fmc-2022-0316 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| PPN (Katalog-ID): |
NLM356736814 |
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| 500 | |a Date Completed 18.05.2023 | ||
| 500 | |a Date Revised 25.05.2023 | ||
| 500 | |a published: Print-Electronic | ||
| 500 | |a Citation Status MEDLINE | ||
| 520 | |a Aim: The objective of the present study is to design and synthesize diverse piperazine-1,2,3-triazole scaffolds as key pharmacophores possessing antimicrobial/anticancer activities. Materials & methods: Twenty-four scaffolds were synthesized via a click-inspired synthetic protocol and were assayed for anticancer activity using the methyl thiazolyl tetrazolium assay and for antimicrobial potency by serial dilution. Results: Among all the tested 1,2,3-triazole scaffolds, compounds 7i (IC50: 5.22 ± 0.05 μM) and 7a (IC50: 5.34 ± 0.13 μM) exhibited good anticancer activity, and 7x also showed notable antimicrobial activity. Molecular docking studies of potent analogs 7i and 7a were performed to provide an insight into their binding interactions. Conclusion: Compound 7x is considered a valuable lead compound for further optimization of anticancer and antimicrobial agents | ||
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| 700 | 1 | |a Yadav, Jyoti |e verfasserin |4 aut | |
| 700 | 1 | |a Singh, Dharmendra |e verfasserin |4 aut | |
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