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Design, synthesis, and biological evaluation of new 1-aryl-4-(β-D-fructopyranos-3-O-yl)methyl-1H-1,2,3-triazole derivatives

Vennam Dinesh Kumar Reddy, Thatipamula Ranjith Kumar, Haridasyam Sharath Babu, Koppula Shiva kumar
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Abstract


New 1-aryl-4-(β-D-fructopyranos-3-O-yl)methyl-1H-1,2,3-triazole derivatives have been synthesized by a CuAAC reaction and their antibacterial and antifungal activity has been evaluated. Some of the derivatives showed remarkable in vitro antibacterial activity against Staphylococcus aureus, Staphylococcus epidermidis, Pseudomonas aeruginosa, and Klebsiella pneumoniae and moderate antifungal activity. In addition, molecular docking studies of these compounds into the active site of Staphylococcus aureus tyrosyl-tRNA synthetase were performed. The docking study revealed that all compounds have considerable binding energies and good affinity toward the active site of the enzyme.


Keywords


arylazide, 1-aryl-4-(β-D-fructopyranos-3-O-yl)methyl-1H-1,2,3-triazoles, 3-O-propargyl-β-D-fructopyranose, antibacterial activity, antifungal activity, click chemistry, molecular docking simulation.

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