Synthesis And Antimicrobial Activities Of 3-(1,2,4-triazolemethyl)-4-Substituted Phenyl-1,5-benzothiazepines

As a class of seven-membered heterocyclic compounds with various biological activities,the 1,5-benzothiazepine compounds occupy a high position in medical research.Some derivatives have been used as drugs for the treatment of mental and cardiovascular diseases.1,2,4-triazole ring is also a class of compounds with many biological activities,some of which were often used as insecticides,herbicides and antifungal drugs in the field of medicine and pesticides.In the early stage of the laboratory,the 1,2,4-triazole ring was introduced into the3-position of 1,5-benzothiazepine seven-membered ring,and the synthesized target had high bacteriostatic activity.According to the principle that "increasing or shortening the carbon chain can improve the pharmacodynamics of the leading compounds",this pape-r has designed and synthesized 3-(1,2,4-triazolemethyl)-4-substituted phenyl of 1,5-benzothiazepines by increasing the carbon chain on the 3-site of the seven-member ring.The antimicrobial activity showed that the compounds maintained the bacteriostatic acti-vity against fungi and bacteria.The expected effect of antimicrobial activity of this kind of compounds was realized.The 3-position carbethoxy substituted 1,5-benzothiazepines have a high inhibitory effect on fungi,the two groups of N,N-dimethylformamide gr-oup and carbethoxy are bioelectron isophora.In this paper,we introduced N,N-dimethylf-ormamide group into the 3-site of 1,5-benzothiazepine seven-membered ring,synthesis of substituted pheny-3-(N,N-dimethylformamide)-4-substituted methyl of 1,5-benzothiazep-ine,The antimicrobial activity showed that the amide substituted compounds maintained a similar inhibitory effect on the tested fungi,but moderately inhibited to the bacteria,showed the opposite biologica activity.The main contents of this thesis are as follows:Firstly,a series of new 3-(1,2,4-triazolomethyl)-4-substituted phenyl-1,5-benzothiazepines derivatives were synthesized from substituted benzene by Fourier acylation reacti-on,Maniche reaction,elimination of addition and six steps reaction.Secondly,substituted 2-phenyl-3-(N,N-dimethylformamide)-4-substituted methyl of 1,5-benzothiazepine was synthesized from N,N-dimethyl acetyl acetamide as raw materialby Knoevenagel condensation and Michael addition and three steps reaction.Thirdly,the structure of the target compound was determined by 1H NMR,13 C NM R,MS,IR and elemental analysis.Lastly,18 kinds of target products of two series were tested for bacteriostatic activity of fungi and bacteria,the structure-activity relationship is discussed.