Chemical and Pharmaceutical Bulletin p. 1760 - 1772 (1991)
Update date:2022-08-05
Topics:
Sato
Dan
Onuma
Tanaka
Aoki
Koga
A series of substituted 7,8-dihydrofuro[2,3-g]-1,2-benzisoxazole-7-carboxylic acids and 7,8-dihydrofuro[2,3-g]benzoxazole-7-carboxylic acids were synthesized and evaluated for uricosuric and diuretic activities in rats. Many of the benzisoxazole derivatives showed uricosuric and only weak diuretic activities, whereas the benzoxazoles exhibited potent diuretic activities with little affecting urate excretion. Among these compounds, 5-chloro-7,8-dihydro-3-phenylfuro[2,3-g]-1,2-benzisoxazole-7-carboxylic acid (AA-193) was found to be a potent uricosuric agent without diuretic activity and was selected for further development.
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