Thia-, Oxa-, and Aza Heterocyclic Derivatives Based on Thiochroman- and Benzothiepine 1,1-dioxide Moieties: Syntheses, Characterization, Antimicrobial-, Antituberculosis-, and Anticancer Activity

Authors

  • P. Palanisamy Department of Chemistry, Manonmaniam Sundaranar University, Tirunelveli-627 012, Tamilnadu, India
  • S. Sudhakar Department of Biotechnology, Manonmaniam Sundaranar University, Tirunelveli-627 012, Tamilnadu, India
  • S. Kumaresan Department of Biotechnology, Manonmaniam Sundaranar University, Tirunelveli-627 012, Tamilnadu, India

Keywords:

Thiochroman, benzothiepine, antimicrobial, antituberclosis, anticancer

Abstract

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 µM. Compounds 9 and 18 were found to exhibit higher cytotoxic potency (15, 13 µM and 14, 12 µM) than that of doxorubicin (21 µM and 19 µM) against HeLa cell and HCT116 cell.

Downloads

Published

2015-05-03

How to Cite

P. Palanisamy, S. Sudhakar, & S. Kumaresan. (2015). Thia-, Oxa-, and Aza Heterocyclic Derivatives Based on Thiochroman- and Benzothiepine 1,1-dioxide Moieties: Syntheses, Characterization, Antimicrobial-, Antituberculosis-, and Anticancer Activity. World Journal of Pharmaceutical Sciences, 3(5), 848–857. Retrieved from https://wjpsonline.com/index.php/wjps/article/view/thia-oxa-aza-heterocyclic-thiochroman-benzothiepine-syntheses

Issue

Section

Research Article