SYNTHESIS OF 1,5-BENZOTHIAZEPINES: PART XXXVII-SYNTHESES AND ANTIMICROBIAL EVALUATION OF 8-SUBSTITUTED-2,5-DIHYDRO-2-(4- METHOXYPHENYL/3,4-DIMETHOXYPHENYL)-4-PHENYL-1,5-BENZOTHIAZEPINES

摘要

Two series of 8-substituted-2,5-dihydro-2-(4-methoxyphenyl/3,4-dimethoxyphenyl)-4-phenyl-1,5-benzothiazepines have been prepared by the reaction of 3-(4-methoxyphenyl)-1-phenyl-2-propenone and 3-(3,4-dimethoxyphenyl)-1-phenyl-2-propenone with six 5-substituted-2-aminobenzenethiols, the substituents being fluoro, chloro, bromo, methyl, methoxy and ethoxy, in dry ethanol saturated with dry HCl gas. All the synthesized compounds were characterized by analytical and spectral data comprising IR, ~1H NMR, ~(13)C NMR, ~(19)F NMR and mass studies. All these compounds have been screened for antimicrobial activity against the gram-positive bacteria, Staphylococcus aureus with standard gatifloxin and the gram-negative bacteria, Pseudomonas aeruginosa with standard natilmicin and the fungus, Candida albicans with standard fluconazole. The antifungal activity was found to be more pronounced than antibacterial.