Chemical and Pharmaceutical Bulletin p. 279 - 286 (1998)
Update date:2022-08-03
Topics:
Tsuji, Kiyoshi
Nakamura, Katsuya
Ogino, Takashi
Konishi, Nobukiyo
Tojo, Takashi
Ochi, Takehiro
Seki, Nobuo
Matsuo, Masaaki
A series of novel 5-substituted-2,3-diarylthiophenes has been synthesized and found to be active in the rat adjuvant arthritis (AA) model and/or in the yeast-induced hyperalgesia (Randall-Selitto) assay. Among the compounds synthesized herein, 2-(4-fluorophenyl)-3-[4- (methylsulfonyl)phenyl]-S-(trifluoromethyl)thiophene (6a) exhibited the most potent activities on AA, collagen-Induced arthritis (CIA) and the delayed- type hypersensitivity response to type II collagen. 5-Bromo-2-[4- (methylamino)phenyl]-3-[4-(methylsulfinyl)phenyl]thiophene (38) is also a potent inhibitor of AA, CIA, hyperalgesia and in vitro tumor necrosis factor- α production.
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