Synthesis and biological evaluation of some bicyclic [2-(2,4-dimethylphenylthio)phenyl] aniline and its amide derivatives as potential antitubercular agents
YOGESH PATIL RAMESH SHINGARE SHAKTI CHAKRABORTY RACHANA BORKUTE DHIMAN SARKAR BALAJI MADJE
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In the present investigation, a series of bicyclic [2-(2,4-dimethylphenylthio)phenyl] aniline analogues were synthesized and characterized by IR,NMR(1H and 13) 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 ReductionMenadione 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 significantantitubercular activity. All the ex vivo active were further evaluated for cytotoxic activity against THP-1, MCK-7 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.
YOGESH PATIL1 RAMESH SHINGARE1 SHAKTI CHAKRABORTY2 RACHANA BORKUTE2 DHIMAN SARKAR2 BALAJI MADJE1
Volume 135, 2023
Continuous Article Publishing mode
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