Synthesis, Characterization and Antibacterial Evaluation of Oxoazetidin ? Benzene Sulfonamide Derivatives as a Hybrid Antimicrobial Agents

Abstract

Ahmed T. Ali, Mazin N. Mosa, Zuhair G. Alshaheen, Munther A. Muhammad-Ali.

Purpose: To preparation of oxoazetidine-benzene sulfonamide conjugates that have the beta lactam and sulfonamide moieties as a possible hybrid antibacterial agent
Method: Eight derivatives of oxoazetidine-benzene sulfonamide have been synthesized by coupling the benzene or toluene with chlorosulfonic acid, and then treated with hydrazine to get hydrazide derivatives. Hydrazide derivatives, then, treated with benzaldehyde derivative to form Schif base intermediate, which will be cyclized with chloroacetyl chloride to obtain the target compounds. The chemical structures had been identified by 1H-NMR, FT-IR and Elemental Analysis and evaluation of their antibacterial activity against Gram-positive, Gram-negative and penicillin-resistant bacteria obtained from clinical specimens using disc diffusion method.
Results: Of these eight compounds, compound 4b4 showed good activity against all types of tested bacteria, compound 4a4 also had a good action against all species tested. Compounds 4a1, 4b1, 4a2, 4b2 showed a greater activity against Gram-negative bacteria as compared to amoxicillin.