Synthesis And Antimicrobial Activities Of2-(1,2,4-triazole)-4-substituted Phenyl-1,5-benzothiazepines Derivatives

1,5-benzothiazepine and its derivatives have been one of the hot areas of humanresearch which have achieved good efficacy in the treatment of cardiovascular diseases,neurological diseases and cancer, and some of its derivatives are well used in agriculture andindustry in recent years. There has long been engaged in the synthesis of1,5-benzothiazepine derivatives and the research of their antimicrobial activities in our laboratory,1,5-benzothiazepine as the basic structural unit by connecting the functional group of theseven-membered ring an ester group, an acyl group, an amide group, a furan and thiopheneetc in oeder to test the antibacterial activity of the target product and selecte the compoundswhich have a better antibacterial activity.1,2,4-triazole compounds have showed good activity in anti-tumor, anti-bacterial andother aspects advance on agriculture as insecticides and herbicides. In view of1,5-benzothiazepine derivatives and1,2,4-triazole both have good physical activity,so the paper2-triazole substituted1,5-benzothiazepine to expect to get some better antibacterial of1,5-benzothiazepines derivatives.The main job in this thesis is as follows:Firstly, the paper used different substituents phenyl and acetyl chloride as startingmaterials, through the Friedel-Crafts acylation reaction, the Mannich reaction, nucleophilicsubstitution reaction, α-H of bromo, hydrogen bromide, and then the Michael addition andintramolecular cyclization reaction six-step to synthesis a series of2-(1,2,4-triazole)-4-substituted phenyl-1,5-benzothiazepines derivatives.Secondly, the structures of these compounds are determined by IR,1H NMR, MS andelemental analysis.Lastly, antimicrobial activities of12novel compounds are researched in vitro throughCryptococcus neoformans and clinical strains of Candida albicans yeast filter paper method,Staphylococcus aureus and Escherichia coli.The test results show that the target compoundsaall have a certain antibacterial activity on above bacterias.