Sulfonamide???lactam Hybrids Incorporating the Piperazine Moiety as Potential Antiinflammatory Agent with Promising Antibacterial Activity

Several monocyclic ?-lactams have been synthesized via a [2+2] ketene–imine cycloaddition reaction (Staudinger reaction) and evaluated for their biological activities. The structure of products was confirmed by spectral data elemental analyses. ?-Lactams 4 b h exhibited 31 27 anti-inflammatory ratios, respectively, which are as well the well-known dexamethasone corticosteroid with 32 ratio. two most active compounds showed IC50 values more than 200 ?M against HepG2 cell line, in comparison doxorubicin (IC50<1 ?M), indicated biocompatibility nontoxic behavior. d, j, k, l, were S. aureus E. coli had broad spectrum property. tested subjected to silico prediction pharmacokinetics properties (ADMET) assess potential vivo effectiveness. molecular docking study that inhibitors fitted iNOS site. This suggests could potentially serve effective inhibitors, represent promising lead treating inflammatory disorders.