2-(Isoxazolylethenyl)phenoxypropanolamines: a new class of .beta.-receptor antagonists with antihypertensive activity
作者:Albrecht Franke、Fritz F. Frickel、Josef Gries、Dieter Lenke、Rainer Schlecker、Peter D. Thieme
DOI:10.1021/jm00144a018
日期:1981.12
potent than labetalol in beta-adrenergic receptor blockade and was effective in lowering blood pressure in acute trials on spontaneously hypertensive rats at a dosage of 15 mg/kg. Structure-activity considerations showed that antihypertensive potency was more sensitive to structural variations than beta-adrenoceptor antagonistic activity. However, in general, those compounds having the most potent beta-adrenoceptor
描述了一系列(E)-1-氨基-3- [2-(2-异恶唑基乙烯基)苯氧基-1-丙醇的合成。发现这些化合物具有β-和α-肾上腺素阻断特性,以及降压和抗高血压特性。所有这些化合物的β-肾上腺素受体拮抗作用均比其α-交感神经和降压活性更为明显。3a在阻断β-肾上腺素能受体方面的功效是拉贝洛尔的16倍,并且在以15 mg / kg的剂量治疗自发性高血压大鼠的急性试验中可有效降低血压。结构活性的考虑表明,降压药效比β-肾上腺素受体拮抗活性对结构变化更敏感。但是,总的来说,