Medicinal Chemistry

Synthesis and Biological Evaluation of Novel 1,4-Disubstituted 1,2,3-Triazoles and Bis 1,2,3-Triazoles as Anti-Bacterial Agents

Abstract

Mumtaz Hussain, Zahid Hussain, Aamer Saeed, Pervaiz Ali Channar, Fayaz Ali Larik, Syeda Aaliya Shehzadi and Tarique Mahmood

A library of novel 1,4-disbustituted 1,2,3-triazoles 3a-3k was prepared by using Click-chemistry concept. In this 1,3-dipolar cycloaddition, the 3-methoxy-4-(prop-2-yn-1-yloxy)benzaldehyde (1) was used as alkyne partner which was synthesized from vanillin and propargyl bromide and was reacted with differently substituted arylpropoxy azides to furnish series of mono and bis 1,4-disubstituted-1,2,3-triazoles. All the synthesized compounds were characterized spectroscopically and were evaluated for their antimicrobial activity. Preliminary results of antibacterial screening revealed that various synthesized compounds have the highest inhibitory effects then the control ciprofloxacin against the growth of a wide range of both gram positive and gram negative bacterial strains. Compounds 3g and 3b were found to be the most active against various strains of gram-positive and gram-negative bacteria.