Synthesis and .beta.-adrenergic blocking activity of a novel class of aromatic oxime ethers
作者:Gerard Leclerc、Andre Mann、Camille Georges Wermuth、Nicole Bieth、Jean Schwartz
DOI:10.1021/jm00222a023
日期:1977.12
A new series of beta-adrenergic blocking amines containing an oximino-propanolic chain linked to an aromatic nucleus was synthesized. Most of the derivatives are characterized by beta2-selectivity. The structure-activity relationship are discussed. One of the compounds, selected for further studies, was more active on the trachea than on the atria of guinea pig, 155 times in vitro and 26 times in vivo
合成了一系列新的β-肾上腺素能阻断胺,它们含有与芳香核相连的肟基-丙醇链。大多数衍生物的特征是β2-选择性。讨论了构效关系。选择用于进一步研究的一种化合物,其对气管的活性高于对豚鼠心房的活性,在体外155倍,在体内26倍。相比之下,丁氧胺的β2选择性在体外为13,而在体内仅为2。使用一系列30种苯乙酮肟衍生物,无法检测到定量的构效关系。