Der Pharma Chemica
Journal for Medicinal Chemistry, Pharmaceutical Chemistry, Pharmaceutical Sciences and Computational Chemistry


Design, synthesis and biological evaluation of substituted 9-oxo-1,2-dihydropyrrolo[2,1-b]quinazolin-3(9H)-ylidene)methyl)piperidine-1-carboxamide derivatives as dual COX-2 and (sEH) inhibitor

Author(s): Vijaykumar Nimbarte

A series of novel dual inhibitor of substituted 9-oxo-1,2-dihydropyrrolo[2,1-b]quinazolin-3(9H)- ylidene)methyl)piperidine-1-carboxamide Derivatives as a pharmacophore lead for Potent antiinflammatory and sEH inhibition have been designed, synthesized and evaluated as novel analogues to act as selective COX-2 Inhibitors over COX-1 which prevent blood pressure elevation by acting as sEH inhibitors in addition. The synthesized compounds 10e and 10g exhibit varying degrees COX-2 selectivity and inhibition of sEH enzyme displaying IC50 values of 0.124±0.011μM and 0.110±0.01μM for in-vitro sEH inhibition respectively