Synthesis and biological activities of optically active 6-[3-(3,4-dimethoxybenzylamino)-2-hydroxypropoxy]-2(1H)-quinolinone (OPC-18790)

被引：0

作者：

Fujioka, T ^{[1
]}

Teramoto, S ^{[1
]}

Tsujimi, S ^{[1
]}

Takemoto, K ^{[1
]}

Mori, T ^{[1
]}

Hosokawa, T ^{[1
]}

Sumida, T ^{[1
]}

Tominaga, M ^{[1
]}

Yabuuchi, Y ^{[1
]}

机构：

[1] OTSUKA PHARMACEUT CO LTD, TOKUSHIMA INST NEW DRUG RES 2, TOKUSHIMA 77110, JAPAN

来源：

CHEMICAL & PHARMACEUTICAL BULLETIN | 1996年 / 44卷 / 08期

关键词：

OPC-18790; optically active epichlorohydrin; cardiotonic agent; 2(1H)-quinolinone; positive inotropic;

D O I：

暂无

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The enantiomers of 6-[3-(3,4-dimethoxybenzylamino)-2-hydroxypropoxy]-2(1H)-quinolinone (OPC-18790), a novel cardiotonic agent, were synthesized and evaluated for positive inotropic activity. The key intermediates, 2,3-epoxypropoxy derivatives, were obtained by the alkylation of 6-hydroxy-2(1H)-quinolinone with optically active epichlorohydrin and subsequent ring closure. In an in vitro study, the (R)-(+)-isomer was about id-fold more potent than the (S)-(-)-isomer.

引用

页码：1596 / 1598

页数：3

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