Synthesis, In-vivo and In-vitro Anti-inflammatory Evaluation of some Novel Coumarin Derivatives

Title:Synthesis, In-vivo and In-vitro Anti-inflammatory Evaluation of some Novel Coumarin Derivatives

Volume: 17 Issue: 2

Author(s): Reem Al-Wabli , Mohammad Fouad and Radwan El-Haggar*

Affiliation:

• Pharmaceutical Chemistry Department, Batterjee Medical College, Jeddah 21442,Saudi Arabia

Keywords: Coumarins, ester derivatives, in-vitro, anti-inflammatory, in-vivo, herbal medicinal, derivatives.

Abstract: 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 COX inhibitors.

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, respectively.

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.

Cite this article as:

Al-Wabli Reem , Fouad Mohammad and El-Haggar Radwan *, Synthesis, In-vivo and In-vitro Anti-inflammatory Evaluation of some Novel Coumarin Derivatives, Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry 2018; 17 (2) . https://dx.doi.org/10.2174/1871523017666180816163448