One-Pot Synthesis of 3-Amino-1,2,4-triazoles Using Choline Chloride-Urea and Their Antibacterial Activities

摘要

In this study, a new one-pot method was proposed for the synthesis of novel and known 3-amino-1,2,4-triazole derivatives in choline chloride/urea (1 : 2) as a biodegradable, nontoxic, biorenewable and inexpensive solvent and reagent. It efficiently catalyzed the reaction between alkyl/aryl hydrazides with urea. Some of the advantages of the proposed method are: eco-friendly and low-cost procedure, easy work-up and purification, good to excellent product yields and acceptable reaction times. This method can be a model for Pellizzari-type reactions. Antimicrobial activity of the synthesized 1,2,4-triazoles were evaluated against five Gram-positive and three Gram-negative pathogenic bacteria via Kirby-Bauer disk diffusion method. Triazoles containing 3-bromophenyl and 4-(tert-butyl)phenyl substituents were the most effective antibacterial agents against all tested bacterial strains.