Synthesis and biological evaluation of some bicyclic [2-(2,4-dimethylphenylthio)phenyl] aniline and its amide derivatives as potential antitubercular agents

TitleSynthesis and biological evaluation of some bicyclic [2-(2,4-dimethylphenylthio)phenyl] aniline and its amide derivatives as potential antitubercular agents
Publication TypeJournal Article
Year of Publication2018
AuthorsPatil, Y, Shingare, R
Tertiary AuthorsChakraborty, S
Subsidiary AuthorsBorkute, R, Sarkar, D, Madje, B
JournalJournal of Chemical Sciences
Volume130
Issue3
Pagination22
Date PublishedFEB
Type of ArticleJournal Article
ISSN9743626
Keywords4-dimethylphenylthio)phenyl] aniline, antituberculosis activity, Cytotoxicity, [2-(2
Abstract

In the present investigation, a series of bicyclic [2-(2,4-dimethylphenylthio)phenyl] aniline analogues were synthesized and characterized by IR, NMR (1H and 13C) and mass spectra. All newly synthesized 15 compounds were inspected for their in vitro antitubercular activity against Mycobacterium tuberculosis (MTB) H37Ra in both active and dormant state using an established XTT Reduction Menadione assay (XRMA). The titled compounds exhibited minimum inhibitory concentration (MIC90) ranging from 0.05 to >30 (μg/mL). The potent four compounds were further evaluated in THP-1 infection model where they demonstrated significant antitubercular activity. All the ex vivo active were further evaluated for cytotoxic activity against THP-1, MCK7 and HeLa cell lines in order to check selectivity index. All compounds were further screened against four different bacteria to assess their selectivity towards MTB. These derivatives could be considered as a precursor structure for further design of antituberculosis agent.

DOI10.1007/s12039-018-1424-5
Type of Journal (Indian or Foreign)

Foreign

Impact Factor (IF)

1.235

Divison category: 
Organic Chemistry