Design, Synthesis and Evaluation of 3-Substituted Coumarin Derivatives as Anti-inflammatory Agents

• DOI: 10.1248/cpb.c19-01085
• Publication Date: 2020-03-12T22:07:07Z
• Authors: Tao Wang; Tao Peng; Xiaoxue Wen; Gang Wang; Shuchen Liu; Yunbo Sun; Shouguo Zhang; Lin Wang
• Keywords: Moiety; Anti-inflammatory

Coumarin moiety has garnered momentous attention especially in the design of compounds with significant biological activities. In this work, a series 3-substituted coumarin derivatives 6a–6l were synthesized and fully characterized. Most could obviously inhibit activity cyclooxygenase-1 (COX-1) at concentration 10 µM. Besides, 6h 6l exhibited highest inhibitory effects against COX-2 inhibition rates 33.48 35.71%, respectively. Detailed structure–activity relationships (SARs) also discussed. vivo studies, 6b, 6i remarkably repress xylene-induced ear swelling mice dose 20 mg/kg. Especially, seemed to be most effective compound mg/kg, displaying favorable anti-inflammatory comparable indomethacin. All these findings suggested that might utilized as candidate for treatment inflammatory diseases.