Thia-, Oxa-, and Aza Heterocyclic Derivatives Based on Thiochroman- and Benzothiepine 1,1-dioxide Moieties: Syntheses, Characterization, Antimicrobial-, Antituberculosis-, and Anticancer Activity
A series of thia-, oxa-, and aza heterocyclic derivatives based on 3,4-dihydro-1-benzothiepin-5(2H)-one 1,1-dioxide, and 2,3-dihydro-4H-thiochroman-4-one 1,1-dioxide moieties were prepared from the diketoesters 2 and 11. All derivatives were evaluated on a few Gram-positive and Gram-negative bacterial strains, as well as the fungal strains. It would also be noticed that the benzodiazepine derivatives 9 and 18 exhibited better antibacterial potentials than the rest. 1,2-Diphenylethane-1,2-diamine substituted thiochromeno- and benzothiepino derivatives 9 and 18 showed good inhibitory activity against MTB (H37Rv) at MIC 7.0 and 6.5 然. Compounds 9 and 18 were found to exhibit higher cytotoxic potency (15, 13 然 and 14, 12 然) than that of doxorubicin (21 然 and 19 然) against HeLa cell and HCT116 cell.
Full Text Attachment