Synthesis of 1,5-benzothiazepines:Part XXXII-Synthesis and antimicrobial studies of 8-substituted-2,5-dihydro-2-(4-pyridyl)-4-(2-thienyl)-1,5-benzothiazepines

摘要

The reactions of 5-substituted-2-aminobenzenethiols,the substituents being F,Cl,Br,CH_3,OCH_3 and OC_2H_5 4a-f,with an alpha,beta-unsaturated heterocyclic ketone,3-(4-pyridyl)-1-(2-thienyl)-2-propenone,have been carried out in dry toluene containing piperidine.The products,8-substituted-2,5-dihydro-2-(4-pyridyl)-4-(2-thienyl)-1,5-benzothiazepines,5a-f,obtained in 65-70% yields,have been characterized by microestimations for C,H,N and IR,~1H NMR and mass spectral studies.The synthesized compounds have been screened for antimicrobial activity against the bacteria Escherichia coli and GFC and fungi,Aspergillus niger,Aspergillus flavus and Curvularia lunata.All the compounds show good antibacterial and antifungal activity.