Novel methylene bridged Mannich bases 2a-j were synthesized in good to excellent yields from the pyrazoline derivative 1 using various primary/secondary amines, 37 % formalin in presence of ionic liquids/TBAB as catalyst. The structures of the newly synthesized compounds were confirmed by IR, 1 H-and 13 C-NMR and GC-MS spectroscopy, as well as elemental analysis. The title compounds were screened for their anti-tubercular and antimicrobial activities. Some of the compounds exhibited very good anti-tubercular, antifungal and antibacterial activities.
Derivatives of 1,3-thiazolidin-2,4-dione appended to biphenyl ring viz., 7-9, 16-18 were prepared. The newly synthesized compounds were confirmed by IR, NMR ( 1 H and 13 C) MS and elemental analyses. Single crystal X-ray diffraction study was carried out for one of the final compounds 9.
An efficient green approach to the synthesis of Schiff bases (11-21) of 1-amino-2-aryl-3-oxo-1,2,4triazoles (1-3) have been reported under Mg(ClO 4) 2 as catalyst followed by the reaction with chloroacetyl chloride in solvent-free conditions to yield the azetidinones (22-32) with excellent yields. The synthesized compounds were evaluated for the extent of penetration into biological membranes (clogP), drug-likeliness and finally drug score was calculated and also screened for antitubercular and antimicrobial activities.
A novel series of Biginelli 2-3 (a and b) and Biginelli-like compounds 4-7 (a and b) were synthesized from 3-aryl-4-formylsydnone 1 (a and b). Since the crystal structure of hyaluronidase was unavailable, the human hyaluronidase protein structure was used as template and homology modeling was performed, validated by Ramachandran plots and subjected to docking studies along with in vitro anti-inflammatory activity assessment against hyaluronidase. Compounds 2-3 (a and b) exhibited potent enzyme inhibition.
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