engleski

Synthesis, structural characterization and antibacterial evaluations of novel 1,2,3-triazole derivatives of benzoxazoles

In the field of drug discovery and development, biologically important heterocycles, such us benzoxazole, known as „privileged structures“ play an important role as promising future drug candidates beacuse of their versatile binding properties for different biotargets.1 Benzoxazole derivatives have shown a wide range of biological activities such as antimicrobial, antiviral, anticancer and antioxidant. The benzoxazole core is part of several drugs such as flunoxaprofen, benoxaprofen, tafaimids, caboxamycinare. 1, 2, 3- triazole is a well-known scaffold that has a widespread occurrence in different compounds due their structural features that enable it to mimic different functional groups as a bioisostere3. Deep eutectic solvents (DES) represents a novel class of green solvents in organic chemistry with high application in many areas. Thus, in this work novel benzoxazole derivatives bearing 1, 2, 3- triazole as a linker were synthesized by Cu(I) catalyzed click reaction of O-propargylated benzoxazoles with corresponding azides in DESs (ChCl/glycerol ; L-carnitine/urea ; D- sorbitol/urea/NH4Cl), Structures of novel compounds were confirmed by 1H- and 13C-NMR spectroscopy. Antibacterial evaluations of novel benzoxazole derivatives were performed on bacterial strains: Escherichia coli, Enterococcus Faecalis, Klebsiella Pneumonia, Pseudomonas aeruginosa and Staphylococcus aureus.

benzoxazole derivatives, deep eutectic solvents, antibacterial evaluations

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