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 mu M) and 7a (IC50: 5.34 +/- 0.13 mu M) 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.

Automated summary

The aim of this study was to design and synthesize diverse piperazine-1,2,3-triazole scaffolds as key pharmacophores with antimicrobial/anticancer activities. Twenty-four scaffolds were synthesized via a click-inspired synthetic protocol and were evaluated for anticancer activity and antimicrobial potency. The results showed that compounds 7i and 7a exhibited good anticancer activity, and compound 7x showed notable antimicrobial activity. Molecular docking studies were conducted to investigate the binding interactions of potent analogs 7i and 7a. Compound 7x is considered a valuable lead compound for further optimization of anticancer and antimicrobial agents.