Syntheses of 1,5-benzothiazepines. Part-XXXIX : Syntheses and antimicrobial studies Of 8-substituted-2,5-dihydro-2-(furan-2-yl)-442-hydroxyphenyl/4-methylphenyl)-1,5-benzothiazepines

摘要

The syntheses of novel twelve 8-substituted,2,5-dihydro-2-(furan-2-yl)-4-(2-hydroxypheny1/4-methylpheny1)-1,5-benzothiazepines have been carried out by the reactions of 5-substituted-2-aminobenzenethiols, the substituents being fluoro, chloro, bromo,. methyl, methoxy or ethoxy, with the enolisable heterocyclic ketones, 3-(furan-2-yl)-1-(2-hydroxyphenyl/4-methylphenyl)-2-propenone in dry ethanol saturated with dry HCl; and characterized by analytical and spectral data comprising IR, H-1 NMR and mass spectral studies. On being screened for antimicrobial activity. against the Gram-positive bacteria, Staphylococcus aureus and Gram-negative bacteria Enterobacter. cloacae, Pseudomonas aeruginosa and fungus, Candida albicans in 36 h duration of incubation,, it was found that the 2-(furan-2-yl)-2,5-dihydro8-methoxy-4-(4-methylphenyl)-1,5-benzothiazepine displayed notable antibacterial activity, one and half times higher than that of Meropenem, against Pseudomonas aeruginosa and good antifungal activity against Candida albicans using Fluconazole as reference standard.