Background: Synthetic coumarin derivatives had attracted considerable attention
for their broad spectrum of biological and pharmacological activities such as; anticoagulant,
antiviral, antibacterial, antitumor and anti-inflammatory activities especially as
Objective: Synthesis of some new coumarin esters using different benzoyl chloride derivatives.
The benzoyl chloride derivatives were selected to have different hydrophobic groups
and this aims to increase the lipophilicity of the final compounds hoping to increase the bioavailability
and thus improve the anti-inflammatory activity.
Methods: The reaction between compound III and different aromatic acyl chloride had resulted
in a series of ester derivatives 1-9. All synthesized new compounds along with compound
III as a parent compound and Celecoxib as a reference, were assessed for their antiinflammatory
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,
Results: All synthesized new compounds 1-9 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 invivo
and in-vitro evaluation.
Conclusion: The newly synthesized ester derivatives 1-9 showed an improved activity
compared with the parent compound III, in both in-vivo and in-vitro screening which
proved that the new ester derivatives improve the activity and/or bioavailability.