Studies on Uricosuric Diuretics: II: Substituted 7,8-Dihydrofuro[2,3-g]-l,2-benzisoxazole-7-carboxylic Acids and 7,8-Dihydrofuro[2,3-g]benzoxazole-7-carboxylic Acids1)

Haruhiko Sato, Takashi Dan, Etsuro Onuma, Haruko Tanaka, Bunya Aoki, Hiroshi Koga

Research output: Contribution to journalArticlepeer-review

12 Citations (Scopus)

Abstract

A series of substituted 7,8-dihydrofuro[2,3-g]-l,2-benzisoxazole-7-carboxylic acids 9 and 7,8-dihydrofuro[2,3-g]benzoxazole-7-carboxylic acids 12 were synthesized and evaluated for uricosuric and diuretic activities in rats. Many of the benzisoxazole derivatives 9 showed uricosuric and only weak diuretic activities, whereas the benzoxazoles 12 exhibited potent diuretic activities with little affecting urate excretion. Among these compounds, 5-chloro~7,8-dihydro-3-phenylfuro[2,3-g]-l,2-benzisoxazole-7-carboxylic acid (9b, AA-193) was found to be a potent uricosuric agent without diuretic activity and was selected for further development.

Original languageEnglish
Pages (from-to)1760-1772
Number of pages13
JournalChemical and Pharmaceutical Bulletin
Volume39
Issue number7
DOIs
Publication statusPublished - 1991

Keywords

  • 2-benzisoxazole-7-carboxylic acid 7
  • 3-g] benzoxazole-7-carboxylic acid
  • 3-g]-l
  • 8-dihydro-furo [2
  • 8-dihydrofuro[2
  • diuretic activity uricosuric activity 7

ASJC Scopus subject areas

  • Chemistry(all)
  • Drug Discovery

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