Syntheses of 1,5-benzothiazepines:Part-XXXIV. Syntheses and antimicrobial studies of 8-substituted-2,5-dihydro-2-(4-methoxyphenyl/3,4-dimethoxyphenyl)-4-(2-thienyl)-1,5-benzothiazepines

摘要

Reactions of the 5-suhstituted-2-aminobenzenethiols 4a-f with the α, β-unsaturated heterocyclic ketones 3a,b were carried out in dry ethanol saturated with dry HCl gas. The products 5a-l were characterized by microestimations for C, H, N, S and 1R, 1H NMR, ~(13)C NMR, ~(19)F NMR and mass spectral studies. The synthesized compounds were screened for antimicrobial activity against the bacteria, Staphylococcus aureus and Pseudomonas aeruginosa and the fungus, Candida albicans. All the compounds showed moderate activity against the bacteria Staphylococcus aureus and Pseudomo-nas aeruginosa with reference to standard drugs, gatifloxin and natilmicin but showed good activity against the fungus, Candida albicans with reference drug fluconazole. The maximum antifungal activity has been shown by the compound 5k having maximum number of methoxyl groups and 5g and 5a having fluoro in addition to methoxyl groups.