CONFORMATIONAL EFFECTS ON THE ACTIVITY OF DRUGS .14. SYNTHESIS AND BETA-ADRENERGIC PROPERTIES OF TETRAHYDRONAPHTHALENE ANALOGS OF DICHLOROISOPROTERENOL

被引：4

作者：

BALSAMO, A

BRESCHI, MC

GIANNACCINI, G

LAPUCCI, A

LUCACCHINI, A

MACCHIA, B

MANERA, C

MARTINI, C

MARTINOTTI, E

NENCETTI, S

ROSSELLO, A

SCATIZZI, R

机构：

[1] UNIV PISA, IST CHIM FARMACEUT & TOSSICOL, I-56126 PISA, ITALY

[2] UNIV PISA, IST POLICATTEDRA DISCIPLINE BIOL, I-56126 PISA, ITALY

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 1993年 / 28卷 / 09期

关键词：

ADRENERGIC DRUGS; BETA-BLOCKING AGENTS; DICHLOROISOPROTERENOL CYCLIC ANALOGS; TETRAHYDRONAPHTHALENE DERIVATIVES;

D O I：

10.1016/0223-5234(93)90034-C

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The tetrahydronaphthalene analogs 4 and 5 of DCI (3b) and of its N-unsubstituted derivative (3a) were synthesized and tested for their beta-adrenergic properties by means of both binding tests and functional tests. Compounds 4 and 5 proved to possess a good affinity for beta-adrenergic receptors accompanied by an appreciable beta-blocking activity, thus indicating that the formal insertion of a beta-blocking drug such as DCI into a tetrahydronaphthalene structure is able to provide compounds which still possess a beta-blocking activity.

引用

页码：735 / 741

页数：7

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[1] CONFORMATIONAL-ANALYSIS OF INTRAMOLECULAR BONDED AMINO ALCOHOLS - CONFORMATIONAL FREE-ENERGIES OF SOME INTRAMOLECULAR OH ... N HYDROGEN-BONDS [J].