151507-20-9Relevant academic research and scientific papers
Studies on anti-inflammatory agents. V. Synthesis and pharmacological properties of 3-(difluoromethyl)-1-(4-methoxyphenyl)-5-[4- (methylsulfinyl)phenyl]pyrazole and related compounds
Tsuji, Kiyoshi,Konishi, Nobukiyo,Spears, Glen W.,Ogino, Takashi,Nakamura, Katsuya,Tojo, Takashi,Ochi, Takehiro,Shimojo, Fumio,Senoh, Hachiro,Matsuo, Masaaki
, p. 1475 - 1481 (2007/10/03)
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.
Pyrazole derivatives, processes for preparation thereof and pharmaceutical composition comprising the same
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, (2008/06/13)
The present invention relates to new pyrazole derivatives represented by the following general formula (I) STR1 wherein R1 is aryl which is substituted with substituent(s) selected from the group consisting of lower alkylthio, cyclo(lower)alkyl
