Abstract

AbstractA 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, 1HNMR, 13C 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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