Synthesis and potential antimicrobial studies on some Mannich bases carrying imidazole moiety

Starting from 2-methyl-4-nitro-imidazole, new 5-(2-methyl-4-nitro-1-imidazomethyl)-1,3,4-oxadiazole-2-thione (3) was synthesized and was subjected to Mannich reaction with appropriate amines to yield a new series of 3-substituted aminomethyl-5-(2-methyl-4-nitro-1-imidazomethyl)-1,3,4-oxadiazole-2-thiones (4a-j). The structure of the title compounds was elucidated by elemental analysis and spectral data. The newly synthesized Mannich bases were screened for their antibacterial and antifungal activity. Many of these compounds exhibited potent antifungal activity

Synthesis, spectral, biological activity, and crystal structure evaluation of novel pyrazoline derivatives having sulfonamide moiety

In the present study, synthesis and characterization of pyrazoline derivatives integrated with sulfonamide scaffold have been performed. The characterization of the molecules was done by elemental analysis, ultraviolet--visible, infrared, nuclear magnetic resonance (NMR), and mass spectra. Crystal structure of compounds 2e and 2g were determined by single crystal X-ray diffraction. In the compounds 2e and 2g, the intra molecular hydrogen bonds N15--H15łdotsO13 and N14--H14łdotsN1 were closed to form a S(6) ring motif, whereas the N14--H14łdotsO17 hydrogen bond links, pairs of molecules related by inversion, forming the familiar R22(10) ring motif. The Hirshfeld surface analysis comprising of the dnorm surface plots, electrostatic potentials and two-dimensional fingerprint plots were generated in order to give visual confirmation of the intermolecular interactions. The molecules were screened for their in vitro antitubercular and antimicrobial activity. The molecules 2n and 2m have shown high potent against M. tuberculosis and most of the molecules have shown good potential against different bacteria and fungi

Synthesis, characterization, crystal structures and biological screening of 4-amino quinazoline sulfonamide derivatives

Three quinazolin-4-ylamino derivatives containing phenylbenzenesulfonamides (7a-7c) were synthesized by reacting (E)-N'-(2-cyanophenyl)-N,N-dimethyl formamidine (6) with different 4- amino-N-(phenyl)benzenesulfonamides (4a-4c) and characterized by different techniques such as HRMS, IR, 1H NMR and 13C NMR spectroscopy. The structural properties were further examined by single crystal X-ray diffraction method. The X-ray data shows that compounds 7a and 7c contain two molecules and 7b contains one molecule in the asymmetric unit. Comparison of conformation of two distinct molecules, “A” and “B”, in the asymmetric unit of 7a and 7c were studied with the aid of reported literature. The in vitro antiproliferative activity of the compounds was tested against two breast cancer cell lines (MDA-MB-231 and MCF7). Compound 7b observed as a highest potent candidate against MDA-MB-231with IC50 of 5.44 µg/mL. Antimicrobial activity was also screened against bacterial and fungal strains. Compound 7a with chloro substitution was observed as the most potent candidate against the Gram-negative bacterial strains, whereas the compounds showed no significant activity against the fungal strain.peerReviewe