Synthesis Characterization and Biological Evaluation of Imidazolo Azatidinone Derivatives

Abstract

Literature reveals that imidazole-azetidine passes a wide range of pharmacological activity. It was also found that 3-chloro-4-oxo azetidine-1-yl)-2-(2-methyl-4,5-diphenyl-1H- Imidazole-1-yl) acetamide derivatives have pharmacological importance. Promoted by the therapeutic importance of imidazole-azetidine one, it was planned to synthesize imidazole- azetidine one derivatives by microwave method and to screen the synthesize for analgesic as well as antimicrobial activity. The compounds plan for synthesis where prepared under available laboratory conditions and were confirmed by physical and spectral. newline2-(2-methyl, 4,5 diphenyl)-1H-Imidazole) was synthesized from Benzene and acetamide in presence of glacial acetic acid and formaldehyde. The synthesized 2-(2-methyl, 4,5 diphenyl)- 1H-Imidazole-1-yl) acetate from 2-(2-methyl, 4,5 diphenyl)-1H-Imidazole) Was reacted with chloromethyl ethyl acetate. For the synthesis of 2-(2-methyl, 4,5 diphenyl)-1H- Imidazole-1-yl) acetahydrazide, 2-(2-methyl, 4,5 diphenyl)-1H-Imidazole-1-yl) acetate reacts with hydrazine hydrate. For synthesis of intermediate Schiff s bases, 2-(2-methyl, 4,5 diphenyl)-1H-Imidazole- 1-yl) acetahydrazide reacts with various aldehyde and formed substituted with various aromatic aldehyde 3-chloro-4-oxo azetidine-1-yl)-2-(2-methyl-4,5- diphenyl-1H-Imidazole-1-yl) acetamide derivatives. newlineThe test drug of all azetidine derivatives 5(a-f) shows significant analgesic activity when compared to that of control in all the three established experimental models of pain. The analgesic activity was maximum at 60 min and 90 min. The possible mechanism is due to decreasing the central sympathetic tone, increase in the release of and#946;-endorphin and enkephalin levels in the spinal cord, increasing the angiotensin 1-7 levels and decreasing newlinexvii newlineThus, to conclude, all azetidine derivative possibly exhibits its analgesic activity both by central analgesic activity (Eddy s hot plate and tail flick) through release of and#946;-endorphin and enkephalins and also peripheral analgesic action (writhing method) through inhibition of COX2 and PGE2 by analgesic activity such as Eddy s hot plate method, Acetic acid induced writhing test, Tail flick method etc. newlineCompound newline