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A new series of 20 benzofuran based sulphonamides was synthesized from salicylaldehyde and ortho-vanillin. Synthesized compounds (VIIIa–VIIIt) were characterized using FT-IR (Fourier-transform infrared spectroscopy), 1H-NMR (Proton nuclear magnetic resonance) and Mass spectroscopic studies. All 20 compounds were subjected to in vitro antitubercular activity against Mycobacterium tuberculosis H37Rv strains. Compounds (VIIIj), (VIIIi), (VIIIo) and (VIIId) were found to exhibit lower MICs (the minimum inhibitory concentrations) as 13, 18, 17 and 19 µg/mL respectively. To predict plausible modes of binding of these compounds, we carried out molecular docking analysis against a target type III polyketide synthase PKS18 from M. tuberculosis (PDB ID: 1TED). [ABSTRACT FROM AUTHOR]

A new series of benzofuran derivatives have been synthesized by the reaction of substituted N-(4-aminophenyl)-1-benzofuran-2-carboxamide with substituted aromatic sulfonyl chlorides in the presence of base with a suitable solvent at 30–100°C temperature and further characterized by Fourier-transform infrared spectroscopy (FT-IR), Proton nuclear magnetic resonance (1H-NMR), elemental analysis and mass spectroscopy studies. All the 26 newly synthesized compounds (Xa–z) were tested for their in-vitro antitubercular (anti-TB) activity against Mycobacterium tuberculosis H37Rv strains. Benzofuran based sulfamides (Xa) and (Xu) were found more potent with the minimum inhibitory concentration (MIC) values 64 µg/mL of each against M. tuberculosis H37Rv; which were then supported by molecular docking studies to gain more insights on the mode of inhibition of M. tuberculosis Polyketide synthase. [ABSTRACT FROM AUTHOR]