BETA-ADRENERGIC BLOCKING AGENTS .6. PRONETHALOL AND PROPRANOLOL ANALOGS WITH ALKYL SUBSTITUENTS IN ALKANOL SIDE CHAIN

被引：22

作者：

HOWE, R

机构：

[1] Imperial Chemical Industries Ltd., Pharmaceuticals Division, Macclesfield, Cheshire, Alderly Park

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 1969年 / 12卷 / 04期

关键词：

D O I：

10.1021/jm00304a019

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Analogs of pronethalol (20) and propranolol (21) with substituents in the amiuoalkanol side chain have been synthesized. Adrenergic β-receptor blocking potency was generally reduced by substituting in the side chain. The erythro isomer of 2-isopropylamino-1-(2-naphthyl)-1-propanol was three times more potent than the threo isomer. Ethyl 2-amino-3-(ethoxyearbonylmethylamino)-3-(2-naphthyl)propionate (27) and 3-ethoxycarbonyl-2-(2-naphthyl)piperazin-5-one (28), obtained as by-products, were formed by self-condensation of the azomethine derived from 2-naphthaldehyde and glycine ethyl ester. © 1969, American Chemical Society. All rights reserved.

引用

页码：642 / &

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