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本文报道儿茶氨基酮Ⅰ_(1～12)及类似物Ⅱ_(1～12)共24个和一个尿嘧啶氨基酮Ⅲ的合成。并对上述化合物的核磁共振谱及质谱进行了讨论。药理研究表明这类化合物对5-HT和Ca~#引起的离体犬肠系膜动脉和基底动脉的收缩无明显对抗作用。某些化合物能增加在体犬股动脉血流量,显示其扩血管作用。其中以Ⅰ_(10)作用最明显,静脉注射后有轻度的降压反应,并能增加麻醉犬的冠状动脉血流量和心肌收缩力,对乌头碱及氯仿诱导的心律失常亦有保护作用。
This article reports the synthesis of 24 and a uracil aminoketone Ⅲ of 24 (superscript th) Aminocetones Ⅰ_ (1 ~ 12) and Ⅱ_ (1 ~ 12) The NMR and mass spectra of the above compounds were also discussed. Pharmacological studies have shown that these compounds on 5-HT and Ca ~ # caused by isolated canine mesenteric artery and basilar artery contraction no significant antagonism. Certain compounds increase blood flow in the canine femoral artery and show vasodilator effects. Among them, Ⅰ_ (10) had the most obvious effect and had a mild antihypertensive response after intravenous injection, and could also increase the coronary blood flow and myocardial contractility in anesthetized dogs and also had a protective effect on aconitine and chloroform induced arrhythmia. .