Design, Synthesis, Antibacterial Evaluation and Docking Studies of Triazole and Tetrazole Linked 1,4-benzodiazepine Nucleus via Click Approach

CHEMISTRYSELECT(2023)

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摘要
A novel series of 1,4-triazole and 1H-tetrazole pharmacophoric motifs embellished analogues linked to the privileged 1,4-benzodiazepine nucleus through an amidophenylene, methylene and phenylene spacer were realized prodigiously through a domino click reaction. The structures of these compounds were established on the basis of their micro analytical IR, (HNMR)-H-1, C-13 NMR and Mass spectral data. A noteworthy feature of this approach, over the variety of other methods available in the literature for the preparation of 1,4-regioisomer of triazole and 1H-tetrazole ring incorporated heterocyclic materials has been their easy access through a one pot strategy of Cu(I) catalyzed cycloaddition of a terminal alkyne with sodium azide. This Cu-catalyzed click approach was applied for the synthesis of triazole and tetrazole incorporated 1,4-benzodiazepine. Further, antibacterial activity and molecular docking studies were also performed to validate their biological potential.
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关键词
Antibacterial activity,Click reaction,Molecular docking,Triazole,Tetrazole
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