CONFORMATIONALLY RESTRAINED BETA-BLOCKING OXIME ETHERS .3. SYNTHESIS AND BETA-ADRENERGIC ANTAGONISTIC ACTIVITY OF DIASTEREOMERIC ANTI AND SYN 5'-(3'-METHYL)ISOXAZOLIDINYL)-N-ALKYLETHANOLAMINES

Authors
BRESCHI MC MACCHIA M MANERA C MICALI E NARDINI C NENCETTI S ROSSELLO A SCATIZZI R
Citation
Mc. Breschi et al., CONFORMATIONALLY RESTRAINED BETA-BLOCKING OXIME ETHERS .3. SYNTHESIS AND BETA-ADRENERGIC ANTAGONISTIC ACTIVITY OF DIASTEREOMERIC ANTI AND SYN 5'-(3'-METHYL)ISOXAZOLIDINYL)-N-ALKYLETHANOLAMINES, European journal of medicinal chemistry, 31(2), 1996, pp. 159-163
Citations number
5
Categorie Soggetti
Chemistry Medicinal
Journal title
European journal of medicinal chemistry → ACNP
ISSN journal
02235234
Volume
31
Issue
2
Year of publication
1996
Pages
159 - 163
Database
ISI
SICI code
0223-5234(1996)31:2<159:CRBOE.>2.0.ZU;2-Z
Abstract
The diastereomeric anti (1d, 2d) and syn (3d, 4d) 5'-(3'-methyl)isoxaz olidinyl)-N-alkylethanolamines were synthesized and assayed for their beta(1)- and beta(2)-adrenergic antagonistic activity by functional te sts on isolated preparations. The pharmacological results, which were compared with those previously obtained for the corresponding isoxazol ine analogs (1d-4d) substituted in the 3'-position with an isopropyl g roup instead of the methyl group in 1d-4d, indicateci that the beta-ad renergic antagonistic activity of the 3'-alkyl-substituted compounds 1 -4 is not substantially influenced by the size of the alkyl substituen t.