2,2-DIALKYLNAPHTHALEN-1-ONES AS NEW POTASSIUM CHANNEL ACTIVATORS

被引：29

作者：

ALMANSA, C

GOMEZ, LA

CAVALCANTI, FL

RODRIGUEZ, R

CARCELLER, E

BARTROLI, J

GARCIARAFANELL, J

FORN, J

机构：

[1] J URIACH & CIA SA,RES CTR,CHEM LABS,DEGA BAHI 59-67,E-08026 BARCELONA,SPAIN

[2] J URIACH & CIA SA,RES CTR,PHARMACOL LABS,E-08026 BARCELONA,SPAIN

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 1993年 / 36卷 / 15期

关键词：

D O I：

10.1021/jm00067a011

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A new series of 2,2-dialkylnaphthalen-1-one potassium channel activators has been prepared, and their in vitro relaxant activities in isolated rat portal vein and guinea pig tracheal spirals as well as their oral antihypertensive effect in spontaneously hypertensive rats have been evaluated. The group of 1,2-dihydro-4-(1,2-dihydro-2-oxo-1-pyridyl)-2,2-dimethylnaphthalen-1-ones with an electron-withdrawing substituent at the 6-position contain the most active compounds and 1,2-dihydro-4-(1,2-dihydro-2-oxo-1-pyridyl)-2,2-dimethyl-1-oxonaphthalene-6-c arbonitrile, 17f (UR-8225), has been selected for further pharmacological development.

引用

页码：2121 / 2133

页数：13

共 39 条

[1] SYNTHESIS OF SOME FUNCTIONALLY SUBSTITUTED BENZOCYCLANONES [J].