Synthesis and activities of oxidative metabolites of the anti-arthritic drug candidate S-2474

We have synthesized and characterized some oxidative metabolites of S-2474. In this study, we discovered a novel skeleton, the 2,3-dihydrobenzofuran derivative, which inhibited PGE 2 production at a very low concentration and was effective in the anti-carrageenin footpad edema assay. This study has...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry 2003-05, Vol.11 (11), p.2415-2419
Main Authors: Inagaki, Masanao, Jyoyama, Hirokuni, Ono, Takashi, Yamada, Katsutoshi, Kobayashi, Mika, Baba, Takahiko, Touchi, Akira, Iwatani, Kouji, Ohkawa, Tomoyuki, Matsumoto, Saichi, Tsuri, Tatsuo
Format: Article
Language:English
Subjects:
Animals
Anti-Inflammatory Agents - chemical synthesis
Anti-Inflammatory Agents - metabolism
Anti-Inflammatory Agents - pharmacology
Benzofurans - chemical synthesis
Benzofurans - pharmacology
Biological and medical sciences
Bones, joints and connective tissue. Antiinflammatory agents
Cyclic S-Oxides - chemistry
Cyclic S-Oxides - metabolism
Cyclic S-Oxides - pharmacology
Dinoprostone - antagonists & inhibitors
Dinoprostone - biosynthesis
Edema - drug therapy
Edema - metabolism
Humans
Interleukin-1 - metabolism
Leukotriene B4 - metabolism
Lipoxygenase Inhibitors
Medical sciences
Microsomes, Liver - metabolism
Pharmacology. Drug treatments
Rats
Thiazoles - chemistry
Thiazoles - metabolism
Thiazoles - pharmacology
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Summary:We have synthesized and characterized some oxidative metabolites of S-2474. In this study, we discovered a novel skeleton, the 2,3-dihydrobenzofuran derivative, which inhibited PGE 2 production at a very low concentration and was effective in the anti-carrageenin footpad edema assay. This study has clarified the primary, major metabolic pathways of antiarthritic drug candidate S-2474.
ISSN:0968-0896
1464-3391
DOI:10.1016/S0968-0896(03)00141-X