Synthesis, Characterization of some new 2,5-disubstituted-1,3,4-Oxadiazole Derived from Diclofenac acid and Evaluation of its Antibacterial Efficacy

Abstract

In this study, some 2,5-disubstituted-1,3,4-oxadiazole compounds derived from Diclofenac acid were synthesized. The work included synthesize of the methyl Diclofenac ester from the Diclofenac acid reaction with excess of absolute methanol (Fischer’s Esterification) and then converting the ester to the Diclofenac acid hydrazide and then reacting the acid hydrazide with some carboxylic acids In the presence of Phosphoryl chloride to obtain offsets 2,5-disubstituted-1,3,4-oxadiazole derivatives (H₄-H₇). Then the compound (H₇) it was possible to react with some primary amines to obtain 2,5-disubstituted-4,3,1-oxadiazole amine compounds. It was diagnosed using FT-IR, ¹H-NMR, ¹³C-NMR and some physical properties. The results of the preliminary evaluation of the biological efficacy against two types of bacteria, the first (Pseudomonas aeruginosa) and the second (Staphylococcus aureus) showed that the synthesized compounds (H₄, H₆, H₁₁, H₁₂) often had an average inhibitory activity against these two types, while it was observed that the compounds (H₇, H₈, H₉, H₁₀) have good inhibition effect against most of them, both compared to the standard inhibitor used.