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Design and Synthesis of (3,5-Disubstituted Isoxazole)-Linked [1,5]-Benzodiazepine Conjugates: Evaluation of their Antimicrobial and Anti-Tyrosinase Activities

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A series of novel 2-(3,5-disubstituted isoxazolyl)-1,5-benzodiazepines and 2,4-bis-(3,5-disubstituted isoxazolyl)-1,5-benzodiazepine derivatives have been designed and synthesised by employing an alkyne/nitrile oxide cycloaddition ‘click’ type chemistry protocol. The structures of the compounds… Click to show full abstract

A series of novel 2-(3,5-disubstituted isoxazolyl)-1,5-benzodiazepines and 2,4-bis-(3,5-disubstituted isoxazolyl)-1,5-benzodiazepine derivatives have been designed and synthesised by employing an alkyne/nitrile oxide cycloaddition ‘click’ type chemistry protocol. The structures of the compounds were determined on the basis of 1H, 13C and 2D-NMR techniques and by HRMS analysis. These hybrid molecules exhibit moderate to significant antimicrobial and anti-tyrosinase activities.

Keywords: design synthesis; anti tyrosinase; antimicrobial anti; benzodiazepine; tyrosinase activities

Journal Title: Journal of Chemical Research
Year Published: 2017

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