REVIEW ANALYSIS ON SYNTHESIS, ENZYME INHIBITION AND HEMOLYTIC STUDY OF NOVEL ACETAMIDE DERIVATIVES

Tóm tắt

The synthesis of 2- (2,4-dichloro-6-{[4-(2-furoyl)-1-piperazine]sulfonyl}phenoxy)-N-(aryl) acetamides was carried out under the controlled conditions as mentioned in the scheme. In the first step, the nucleophile is formed by reacting the calculated amount of N-(2-furoyl) piperazine (1) with 3,5-dichloro-2- hydroxybenzenesulfonylchloride (2) in the presence of an aqueous solution of sodium carbonate and stirred for three hours at room temperature to produce{4-[(3,5-dichloro-2-hydroxyphenyl)sulfonyl]-1- piperazinyl}(2-furoyl)methanone (3). In the parallel set of reactions, electrophile was prepared by reacting substituted aniline with acetyl bromide in the vicinity of an aqueous sodium carbonate solution. Vigorous shaking formed the precipitates of the electrophile. In the final step, nucleophile and electrophile reacted with each other in an acetonitrile/K2CO3 medium that produced various 2-(2,4-dichloro-6-{[4-(2-furoyl)-1-piperazine] sulfonyl}phenoxy)-N-(aryl) acetamides (7a-c) as outlined in scheme-1. Their structures are confirmed by spectral analysis techniques such as EI-MS, Infrared (IR), proton, and 13C NMR. The synthesized compounds' enzyme inhibition potential was tested against a-glucosidase, AChE, and BChE enzymes. As illustrated from the results of IC50, these compounds are observed as the active inhibitory potential for these enzymes. The cytotoxic activity by hemolytic Assay revealed that these compounds have mild exposure to cytotoxicity on RBCs.