Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10592942 | Bioorganic & Medicinal Chemistry Letters | 2014 | 5 Pages |
Abstract
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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Authors
Hyeon-Lok Jang, Mohammed I. El-Gamal, Hye-Eun Choi, Ho-Yeong Choi, Kyung-Tae Lee, Chang-Hyun Oh,