Conformationally restrained beta-blocking oxime ethers .3. Synthesis and beta-adrenergic antagonistic activity of diastereomeric anti and syn 2-(5'-(3'-methyl)isoxazolidinyl)-N-alkylethanolamines

被引：7

作者：

Breschi, MC ^{[1
]}

Macchia, M ^{[1
]}

Manera, C ^{[1
]}

Micali, E ^{[1
]}

Nardini, C ^{[1
]}

Nencetti, S ^{[1
]}

Rossello, A ^{[1
]}

Scatizzi, R ^{[1
]}

机构：

[1] UNIV PISA,DIPARTIMENTO SCI FARMACEUT,I-56100 PISA,ITALY

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 1996年 / 31卷 / 02期

关键词：

adrenergic drug; beta-blocking agent; 2-(5'-isoxazolidinyl)ethanolamine;

D O I：

10.1016/0223-5234(96)80449-1

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The diastereomeric anti (1d, 2d) and syn (3d, 4d) 2-(5'-(3'-methyl)isoxazolidinyl)-N-alkylethanolamines were synthesized and assayed for their beta(1)- and beta(2)-adrenergic antagonistic activity by functional tests on isolated preparations. The pharmacological results, which were compared with those previously obtained for the corresponding isoxazoline analogs (1d-4d) substituted in the 3'-position with an isopropyl group instead of the methyl group in 1d-4d, indicateci that the beta-adrenergic antagonistic activity of the 3'-alkyl-substituted compounds 1-4 is not substantially influenced by the size of the alkyl substituent.

引用

页码：159 / 163

页数：5

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