Wu E S, Cole T E, Davidson T A, Blosser J C, Borrelli A R, Kinsolving C R, Milgate T E, Parker R B
J Med Chem. 1987 May;30(5):788-92. doi: 10.1021/jm00388a007.
The synthesis of a series of (3-phenylflavonoxy)propanolamines is described. These compounds were evaluated for potential antihypertensive activity in spontaneously hypertensive rats, as well as for in vivo and in vitro evidence of beta-adrenoceptor antagonism. Some of the compounds of this series exhibited effective antihypertensive properties but did not antagonize beta-adrenergic receptors. These active compounds represent a unique series of effective antihypertensive agents that, despite possessing structural characteristics typical of beta-blockers, does not have beta-adrenergic receptor blocking activity.
本文描述了一系列(3-苯基黄酮氧基)丙醇胺的合成。对这些化合物在自发性高血压大鼠中进行了潜在降压活性评估，以及进行了体内和体外β-肾上腺素能受体拮抗作用的研究。该系列中的一些化合物表现出有效的降压特性，但不拮抗β-肾上腺素能受体。这些活性化合物代表了一类独特的有效抗高血压药物，尽管具有β-阻滞剂的典型结构特征，但不具有β-肾上腺素能受体阻断活性。
