Synthesis of tricyclic fused coumarin sulfonates and their inhibitory effects on LPS-induced nitric oxide and PGE2 productions in RAW 264.7 macrophages
- Synthesis of tricyclic fused coumarin sulfonates and their inhibitory effects on LPS-induced nitric oxide and PGE2 productions in RAW 264.7 macrophages
- 장현록; 모하메드엘가말; 최혜은; 최호영; 이경태; 오창현
- Antiinflammatory; Coumarin; Nitric oxide; PGE2; Sulfonate; Tricyclic fused coumarin
- Issue Date
- Bioorganic & medicinal chemistry letters
- VOL 24, NO 2, 571-575
- The regulations of NO and PGE2 productions are research topics of interest in the field of antiinflammatory
drug development. In the present study, a series of tricyclic fused coumarin sulfonate derivatives
was synthesized and evaluated for their abilities to inhibit NO and PGE2 productions in LPS-induced
RAW 264.7 macrophages. Among all the target compounds, compound 1g possessing p-(trifluoromethyl)
phenyl and fused cycloheptane moieties showed the highest inhibitory effects on NO and PGE2
productions. Compound 1g not only inhibited COX-2 activity but also reduced expressions of COX-2
and iNOS. Furthermore, ADME profiling showed that compounds 1g, 1j, 1m, and 1n are estimated to
be orally bioavailable.
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