Synthesis, antimicrobial activities and GAPDH docking of novel 1, 2, 3-triazole derivatives

Purpose: To synthesize new triazole derivatives in order to overcome the problem of side effects antimicrobial agents and microbial resistance, while broadening spectrum activity.
 Methods: The starting triazole, compound 1, was prepared through click chemistry reacted with chloroacetyl chloride yield II. Triazole 1 acids aldehydes produce oxadiazole (III) azomethine (IV) which cyclized acetic anhydride give a acetylated (V). Minimum inhibitory concentration (MIC) resorufin assays were used for antibacterial anti-parasitic screening, respectively. Compounds II IVb subjected molecular docking studies using glyceraldehyde-3-phosphate dehydrogenase (GAPDH) Molecular Operating Environment (MOE) program.
 Results: Novel oxazole-triazole derivative showed high activity against Pseudomonas aeruginosa moderate Staphylococcus epidermidis, whereas IVc epidermidis. Chloro-acetyl-triazole 2-hydroxyphenyl-triazole Schiff base (Ivb) pronounced kinetoplastid parasites, Leishmania major, mexicana Trypanosoma brucei.
 Conclusion: synthesized triazoles represent scaffold identifies potential lead compounds follow-up further mechanistic studies.