Chemical and Pharmaceutical Bulletin p. 1475 - 1481 (1997)
Update date:2022-08-05
Topics:
Tsuji, Kiyoshi
Konishi, Nobukiyo
Spears, Glen W.
Ogino, Takashi
Nakamura, Katsuya
Tojo, Takashi
Ochi, Takehiro
Shimojo, Fumio
Senoh, Hachiro
Matsuo, Masaaki
A series of novel 1,5-diphenylpyrazole derivatives hearing hydrophilic substituents was prepared. The anti-inflammatory and analgesic activities of these compounds were evaluated by using the adjuvant arthritis and Randall- Selitto assays in rats, and the structure-activity relationships were studied. The optimal compound was 3-(difluoromethyl)-1 -(4-methoxyphenyl)-5- [4-(methylsulfinyl)phenyl]pyrazole (10) with oral Ed50 values of 0.31 and 2.6mg/kg on adjuvant-induced arthritis and carrageenin-induced foot edema, respectively. Compound 10 showed analgesic activities not only toward inflamed paw but also toward normal paw (ED30=0.55 and 1.8mg/kg, respectively) in the Randall-Selitto assay, and moreover, 10 was effective in the tail-pinch assay (ED50=21 mg/kg) similarly to morphine. The asymmetric synthesis and pharmacological properties of the enantiomers of 10 are also reported.
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