Synthesis and Pharmacological Evaluation of 6-(7-Theophylline)-3(2H)-Pyridazinone: Synthese und Pharmakologische Prüfung von 6-(7-Theophyllin) 3(2H)-pyridazinon
作者:Stefano Corsano、Giovannella Strappaghetti、Rosano Ferrini、Nara Giglioli
DOI:10.1002/ardp.2503241212
日期:——
PDE-inhibitors and cardiac stimulants, some of them being several times more active than theophylline. A variety of 4,5-dihydro-6-phenyl-3(2H)-pyridazinone derivatives are PDE-inhibitors like CI-914 (2) which produced a cardiotonic effect accompanied by only slight decreases in blood pressure and moderate increases in heart rate. In a recent report some 6-phenyl-3(2H)-pyridazinones showed a bronchospasmolytic
自从茶碱 (1) 作为第一个用于治疗哮喘的 PDE 抑制剂被引入以来,该治疗领域一直在积极地设计具有更高效力和功效的药物。茶碱和其他嘌呤类似物的衍生物被制备和测试作为 PDE 抑制剂和心脏兴奋剂,其中一些比茶碱的活性高几倍。各种 4,5-二氢-6-苯基-3 (2H) -哒嗪酮衍生物是 PDE 抑制剂,如 CI-914 (2) 产生强心作用,伴有血压轻微下降和心率适度增加. 在最近的一份报告中,一些 6-苯基-3 (2H) -哒嗪酮显示出比黄嘌呤更显着的支气管痉挛作用。在本文中,我们报告了 6- (7-茶碱) -3 (2H) -哒嗪酮的合成和药理学特征;