Studies On The Synthesis And Antimicrobial Activities Of3-(1,2,4-triazole)-4-substituted Phenyl-1,5-benzothiazepines

Because1,5-benzothiazepine have a variety of biologically actives, making sucha high position in material possessions clinical studies. These compounds not only totreat mental disorders, also commonly used in the treatment of cardiovascular disease.Recent studies have found that1,5-benzothiazepine drug also has anti-HIV,anti-bacterial and anti-fungal and other efficacy.There has long been engaged in the synthesis of1,5-benzothiazepine derivativesand the research of their antimicrobial activities in our laboratory. Test results of theantimicrobial activity show that some of these compounds have good antimicrobialeffects on Candida albicans, which will have important significance to find the newphysiological activity and special function of drugs.1,2,4-triazole has antiseptic,insecticide, anti-oxidation, anti-cancer and other biologically active.It also has thecharacteristics of high efficiency and low toxicity. Given the role of both1,5-benzothiazepine and1,2,4-triazole.3-triazole substituted1,5-benzothiazepinesare synthesized hopes to put together two different groups to achieve betterpharmacodynamic activity and get better antibacterial activity of the compounds.The main job in this thesis is as follows:Firstly, a series of new3-(1,2,4-triazole)-4-substituted phenyl-1,5–benzothiazepine are synthesized by the Friedel-Crafts acylation reaction, Bromination reaction, Nucleophilic substitution reaction, Mannich reaction and Michael addition reaction, which different substituted benzene and acetylchloride are used for theraw materials.Secondly, The prepared12kinds of3-(1,2,4–triazole)-4-substituted phenyl-1,5-benzothiazepines analyzed by IR、1H NMR、MS and elemental determine itsstructure.Lastly, antimicrobial activities of these novel compounds are researched in vitro.The test results show that the series of compounds in New cryptococcus clinicalstrains and Esherichia coli has good activity.