Studies on uricosuric diuretics. II. Substituted 7,8-dihydrofuro[2,3-g]-1,2-benzisoxazole-7-carboxylic acids and 7,8-dihydrofuro[2,3-g]benzoxazole-7-carboxylic acids

DOI: 10.1248/cpb.39.1760

Source and publish data:

Chemical and Pharmaceutical Bulletin p. 1760 - 1772 (1991)

Update date:2022-08-05

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Authors:

Sato Sato

Dan Dan

Onuma Onuma

Tanaka Tanaka

Aoki Aoki

Koga Koga

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Article abstract of DOI:10.1248/cpb.39.1760

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.

Full text of DOI:10.1248/cpb.39.1760

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