具有促尿酸排泄活性的芳氧基乙酸类利尿剂。II. 取代的[(4-氧代-4H-1-苯并吡喃-7-基)氧基]乙酸及其相关化合物。

Aryloxyacetic acid diuretics with uricosuric activity. II. Substituted [(4-oxo-4H-1-benzopyran-7-yl)oxy]acetic acids and the related compounds.

作者信息

Kitagawa M, Yamamoto K, Katakura S, Kanno H, Yamada K, Nagahara T, Tanaka M

机构信息

Research Institute, Daiichi Pharmaceutical Co., Ltd., Tokyo, Japan.

出版信息

Chem Pharm Bull (Tokyo). 1991 Oct;39(10):2681-90. doi: 10.1248/cpb.39.2681.

DOI:10.1248/cpb.39.2681

PMID:1806291

Abstract

Di- and tri-substituted [(4-oxo-4H-1-benzopyran-7-yl)oxy]acetic acids, and 4-oxo-3-phenyl-4H-furo[2,3-h]-[1]benzopyran-8-carboxylic acid were synthesized and tested for natriuretic and uricosuric activities. Among the compounds tested, 3,5-disubstituted [(4-oxo-4H-1-benzopyran-7-yl)oxy]acetic acids (6c-f, h, n and x) showed potent natriuretic and uricosuric activities, whereas 4-oxo-3-phenyl-4H-furo[2,3-h][1]benzopyran-8-carboxylic acid (6dd) possessed only potent natriuretic activity. The structure-activity relationships are also discussed.

摘要

合成了二取代和三取代的[(4-氧代-4H-1-苯并吡喃-7-基)氧基]乙酸以及4-氧代-3-苯基-4H-呋喃并[2,3-h]-[1]苯并吡喃-8-羧酸，并对其利尿和促尿酸排泄活性进行了测试。在所测试的化合物中，3,5-二取代的[(4-氧代-4H-1-苯并吡喃-7-基)氧基]乙酸（6c-f、h、n和x）表现出强效的利尿和促尿酸排泄活性，而4-氧代-3-苯基-4H-呋喃并[2,3-h][1]苯并吡喃-8-羧酸（6dd）仅具有强效的利尿活性。还讨论了构效关系。