Synthesis of oxypropanolamine derivatives of 3, 4-dihydro-2H-1, 4-benzoxazine, β-adrenergic affinity, inotropic, chronotropic and coronary vasodilating activities

…, G Bruni, MR Romeo, P Massarelli, S Teramoto…

Index: Iakovou, Kriton; Kazanis, Michalis; Vavayannis, Andreas; Bruni, Giancarlo; Romeo, Maria Raffaella; Massarelli, Paola; Teramoto, Shuji; Fujiki, Hiroyuki; Mori, Toyoki European Journal of Medicinal Chemistry, 1999 , vol. 34, # 11 p. 903 - 917

Full Text: HTML

Citation Number: 21

Abstract

Aseries of oxypropanolamine derivatives of 3, 4-dihydro-2H-1, 4-benzoxazine were synthesized and evaluated for inotropic, chronotropic and coronary vasodilating activities in the canine heart, affinity to β1-adrenergic receptor in turkey erythrocytes and affinity to the β2- adrenergic receptor in the rat lung. Among these compounds, 4-acetyl-6-(3-tert-butylamino-2- hydroxy) propoxy-3, 4-dihydro-2H-1, 4-benzoxazine showed 2.1-fold more potent affinity ...