STUDIES ON HINDERED PHENOLS AND ANALOGS .2. 1,3-BENZOXATHIOLES HAVING SRS-A INHIBITING ACTIVITY

被引：24

作者：

AIZAWA, Y

KANAI, T

HASEGAWA, K

YAMAGUCHI, T

IIZUKA, Y

IWAOKA, T

YOSHIOKA, T

机构：

[1] SANKYO CO LTD,MED CHEM RES LABS,2-58 HIROMACHI 1 CHOME,SHINAGAWA KU,TOKYO 140,JAPAN

[2] SANKYO CO LTD,NEW LEAD RES LABS,SHINAGAWA KU,TOKYO 140,JAPAN

[3] SANKYO CO LTD,BIOL RES LABS,SHINAGAWA KU,TOKYO 140,JAPAN

[4] SANKYO CO LTD,ANALYT & METAB RES LABS,TOKYO 140,JAPAN

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 1990年 / 33卷 / 05期

关键词：

D O I：

10.1021/jm00167a032

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of hindered phenolic 1,3-benzoxathioles (7a-1) were prepared and investigated for biological properties. Many compounds had LPO-lowering, antisuperoxide inhibiting, SRS-A inhibiting, and 5-lipoxygenase inhibiting activities. Among them, 5-hydroxy-4,6,7-trimethyl-2-propyl-l,3-benzoxathiole (7d) and 3-(5-hydroxy-4,6,7-tri-methyl-l,3-benzoxathiol-2-yl)propanol (7j) were most potent in SRS-A inhibiting and 5-lipoxygenase inhibiting activities, respectively, and were selected for further development as candidate drugs for the treatment of asthma. © 1990, American Chemical Society. All rights reserved.

引用

页码：1491 / 1496

页数：6

共 37 条

[1]

ASAYAMA K, 1984, DIABETES, V3, P160

[2]

CHAIT A, 1986, ATHEROSCLEROSIS, V7, P491

[3] SYNTHESIS OF 5-HYDROXY-1,3-BENZOXATHIOLE [J].

DEGANI, I ;

DOLCI, M ;

FOCHI, R .

SYNTHETIC COMMUNICATIONS, 1980, 10 (02) :161-166

[4]

FEARS R, 1984, DRUG TODAY, V20, P257

[5]

HASEGAWA K, UNPUB

[6] PHARMACOLOGICAL PROPERTIES OF A NEW ANTI-INFLAMMATORY COMPOUND, ALPHA-(3,5-DI-TERT-BUTYL-4-HYDROXYBENZYLIDENE)-GAMMA-BUTYROLACTONE (KME-4), AND ITS INHIBITORY EFFECTS ON PROSTAGLANDIN SYNTHETASE AND 5-LIPOXYGENASE [J].

HIDAKA, T ;

HOSOE, K ;

ARIKI, Y ;

TAKEO, K ;

YAMASHITA, T ;

KATSUMI, I ;

KONDO, H ;

YAMASHITA, K ;

WATANABE, K .

JAPANESE JOURNAL OF PHARMACOLOGY, 1984, 36 (01) :77-85

[7]

ISOMURA Y, 1984, CHEM PHARM BULL, V32, P152

[8]

IWAOKA T, 1988, ROLE OXYGEN CHEM BIO, P461

[9]

KATSUMI I, 1986, CHEM PHARM BULL, V34, P121

[10]

LUNDBERG WO, 1962, AUTOOXIDATION ANTIOX, V2

← 1 2 3 4 →