Synthesis, in-vivo and in-vitro Anti-inflammatory Evaluation of some Novel Coumarin Derivatives.
Cuvinte cheie
Abstract
The promising activity of coumarin derivatives as anti-inflammatory agents has motivated us to synthesize a new series of coumarin derivatives aiming to improve the anti-inflammatory activity and/or bioavailability. In the present work, the reaction between compound III and different aromatic acyl chloride had resulted in a series of ester derivatives 1-9. All synthesized new compounds 1-9 along with compound III as a parent compound and Celecoxib as a reference, were assessed for their anti-inflammatory activity both in-vivo and in-vitro using the formalin-induced hind paw edema method and inhibition of albumin denaturation and red blood cells (RBCs) membrane stabilization, respectively. All compounds showed an improved activity compared with the parent compound III, in both in-vivo and in-vitro screening. In addition, compounds, 1, 5, 6, 7 and 8 showed significant anti-inflammatory activity compared with the standard compound Celecoxib with compound 6 has a comparable activity with Celecoxib in both in-vivo and in-vitro evaluation.