Fenbufen, a New Anti-Inflammatory Analgesic: Synthesis and Structure-Activity Relationships of Analogs

Autor: Child, Ralph G., Osterberg, Arnold C., Sloboda, Adolph E., Tomcufcik, Andrew S.
Zdroj: Journal of Pharmaceutical Sciences; April 1977, Vol. 66 Issue: 4 p466-476, 11p
Abstrakt: One hundred analogs of fenbufen were prepared and tested using the carrageenan, polyarthritis, and UV erythema anti-inflammatory tests and the 2-phenyl-l,4-benzoquinone writhing and inflamed paw pressure analgesic tests. Only three retained the same full spectrum of activity as fenbufen: dl-4-(4-biphenylyl)-4-hydroxybutyric acid, dl-4- (4-biphenylyl)-l,4-butanedio), and 4-biphenylacetic acid. Fenbufen had the same spectrum of activity as aspirin, phenylbutazone, and indo- methacin in the five tests. In addition, dose-response derived potencies show fenbufen more potent than aspirin and at least as potent as phenylbutazone in all five tests. Two related compounds were generally similar.
Databáze: Supplemental Index