Synthesis, Antimicrobial and Antioxidant Activity of Pyrazole Based Sulfonamide Derivatives.

A series of new sulfonamides have been synthesized from Ampyrone with different benzene sulfonyl chlorides to yield the N-1,5-dimethyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazol-4-yl) benzenesulfonamides (4a-e). All synthesized compounds were characterized on the basis of FTIR, 1H NMR, and 13C NMR, and also by the aid of mass spectral data. Further, all synthesized compounds have studied for their in vitro antimicrobial activities against selected bacterial as well as fungal strains by the agar well diffusion method. Free radical scavenging activity has been investigated by using DPPH method. Among all the synthesized compounds, 4b, 4d, and 4e exhibited significant antimicrobial and antioxidant activities.

Prediction of theoretical physicochemical properties and one-pot synthesis of bis-azetidinones by [2+2] ketene--imine cycloaddition in the presence of montmorillonite.

A simple, highly efficient and environmentally friendly microwave accelerated one-pot synthesis of a series of differently substituted bis-azetidinones have been synthesized expeditiously in good yields from 1,2-diaminoethane and aromatic aldehydes in the presence of zeolite. The structures of the newly synthesized compounds were confirmed by IR, NMR, and mass spectra. The design and calculated molecular properties of all the reported compounds are on the basis of hypothetical antibacterial pharmacophores, which were formulated to interact with microorganisms. A correlation of structure and activity relationship of these compounds with respect to Lipinski rules and drug likeness properties of drugs are described and verified experimentally.