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

Authors
BALSAMO A BRESCHI MC GIANNACCINI G LAPUCCI A LUCACCHINI A MACCHIA B MANERA C MARTINI C MARTINOTTI E NENCETTI S ROSSELLO A SCATIZZI R
Citation
A. Balsamo et al., CONFORMATIONAL EFFECTS ON THE ACTIVITY OF DRUGS .14. SYNTHESIS AND BETA-ADRENERGIC PROPERTIES OF TETRAHYDRONAPHTHALENE ANALOGS OF DICHLOROISOPROTERENOL, European journal of medicinal chemistry, 28(9), 1993, pp. 735-741
Citations number
38
Categorie Soggetti
Chemistry Medicinal
Journal title
European journal of medicinal chemistry → ACNP
ISSN journal
02235234
Volume
28
Issue
9
Year of publication
1993
Pages
735 - 741
Database
ISI
SICI code
0223-5234(1993)28:9<735:CEOTAO>2.0.ZU;2-E
Abstract
The tetrahydronaphthalene analogs 4 and 5 of DCI (3b) and of its N-uns ubstituted derivative (3a) were synthesized and tested for their beta- adrenergic properties by means of both binding tests and functional te sts. Compounds 4 and 5 proved to possess a good affinity for beta-adre nergic receptors accompanied by an appreciable beta-blocking activity, thus indicating that the formal insertion of a beta-blocking drug suc h as DCI into a tetrahydronaphthalene structure is able to provide com pounds which still possess a beta-blocking activity.