Der Pharma Chemica
Journal for Medicinal Chemistry, Pharmaceutical Chemistry, Pharmaceutical Sciences and Computational Chemistry


One pot synthesis of (1-aryl-1H-1, 2, 3-triazol-4-yl) methyl esters of L-aminoacids and their biological activity

Author(s): Rajender Orsu, Sirassu Narsimha, Althaf Hussain, Vasudeva Reddy Nagavelli

A flexible method for the synthesis of new derivatives of 1, 2, 3-triazoles consisting of natural amino acids are described. The triazole derivatives were synthesized from various aromatic azides, proporgyl bromide and naturally available L-aminoacids. The N- protected L-aminoacids converted into O-propargyl esters and they were subjected to copper catalyzed 1,3-dipolar cycloaddition reactions with various aromatic azides. These novel 1,4-disubtituted 1,2,3-triazoles exhibited highly potent activity against bacterial organisms and molecular docking studies revealed the close proximity between the protein receptor and the newly synthesized ligands. And also exhibited moderate anticancer activity and partial DNA Cleavage activity.