A novel series of pyrazole bearing [1,2,4]triazolo [3, 4-b] [1,3,4] thiadiazole derivatives (6 a-l) such as 3-(5-(3-fluoro-4-methoxyphenyl)-1H-pyrazol-3-yl)-6-(2-methoxyphenyl)- [1,2,4]triazolo [3, 4-b] [1,3,4]thiadiazole were synthesized by cyclo-condensation of 4-amino-5-[5-(3-fluoro-4-methoxy-phenyl)-1H-pyrazol-3yl]-4H-[1, 2,4]triazole-3-thiol (5) with substituted benzoic/pyridinyl acids in phosphorus oxychloride giving good yields and purity. IR, 1 H NMR, 13 C NMR and LCMS/MS spectroscopy were used to characterise all the synthesized compounds. All the new derivatives were appraised for their antimicrobial activity, antifungal assay against C. Albicans, A. Niger and A. Clavatus along with Nystatin and Griseofulvin as standard drug and antibacterial assay against E. Coli, P. Aeruginosa, S. Aureus, S. Pyogenus along with Ampicillin as standard drug. Compounds (6 b) and (6 j) displayed excellent antifungal activity whereas compound (6 d) and (6 e) displayed excellent antibacterial activity. Molecular modelling and adsorption, distribution, metabolism and excretion-toxicity (ADMET) prediction data clearly shows that 1,2,4-triazolo[3, 4-b][1, 3,4] thiadiazole derivatives (6 a-l) have potential to explore in the drug discovery pipeline as antifungal agents.

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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 (1 H and 13 C) and mass spectra. All newly synthesized 15 compounds were inspected for their in vitro antitubercular activity against Mycobacterium tuberculosis (MTB) H 37 Ra 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, 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.

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