Synthesis And Biological Evaluation Of Substituted Phenyl Azetidine Phenyl Thiazolidin 2 One Sulfonyl Derivatives

Abstract

newline Background: From many decades heterocyclic compounds containing azetidine, thiazolidines newlineand sulphonamide ring are important targets in synthetic and medicinal chemistry. The problem newlineof antibiotic resistance is now recognized as a serious threat and it needs to be addressed newlineseriously. Microorganisms have mutated and resulted in the generations of multidrug-resistant newline(MDR) and current generation of antibiotics has become ineffective. From literature survey it newlinewas also revealed that azetidine, thiazolidines and sulphonamide ring is present in versatile newlineantimicrobial agents. In view of above mentioned context I have tried to synthesize, characterize newlineand evaluate their antimicrobial and anti-viral potential. Method: Substituted aromatic aldehydes newlinereacted with benzenesulphonamide yielded N-[(E)-(R-phenyl) methylidene]-4- newlinemethylbenzenesulfonamide derivatives (3a-3t). In the next step 4-(R-phenyl)-3-chloro-1-[(4- newlinemethylphenyl) sulfonyl]azetidin-2-one derivatives (5a 5t) were prepared by the treatment of (3a newline3t) with chloroacetyl chloride. Further (3a 3t) derivatives were reacted with thioglycolic acid to newlineobtain a series of 2-(R-phenyl)-3-[(4- methylphenyl) sulfonyl]-1,3-thiazolidin-4-one derivatives newline(7a 7t). These derivatives were tested for their antimicrobial activity by agar disc diffusion newlinemethod and MIC, also screened for in-vitro Anti-viral activity. The spectral study confirmed the newlinesynthesis of desired compounds meant for study. Results: Interestingly, compound 5d, 5e, 5f, newline5h, 5i, and 5j showed similar or better antibacterial activity as compared to ampicillin (standard newlinedrug). Moreover, compounds 5h, 5i, 5j, and 5q showed good inhibitory activity against fungal newlinestrains. The result of the anti-microbial assay demonstrated compounds 7d, 7f, 7g, 7h, 7i, 7j newlineshowed prominent inhibitory activity against all the tested Gram-positive and Gram-negative newlinebacterial strains, while compounds 7g, 5j, 7o, 7p, 7q showed significant activity against the newlineentire set of fungal strains as compared to stand