吡嗪咪唑啉类化合物的结构与α-肾上腺素能活性
Structure and alpha-adrenergic activity of pyrazinimidazolines.
作者信息
Kaliszan R, Damasiewicz B, Nasal A, Radwańska A, Foks H, Kuźmierkiewicz W, Pancechowska-Ksepko D, Rudnicka K, Wisterowicz K, Ośmiałowski K
出版信息
Agents Actions. 1985 Jul;16(5):435-42. doi: 10.1007/BF01982885.
The effects of newly synthetized pyrazinimidazolines on the contraction of isolated rat tail artery and on the chronotropic action of rat atria as well as the effects on blood pressure in anaesthetized rats were determined. The structure-activity relationships were studied, including standard imidazoline drugs. Starting from practically inactive derivatives the step-by-step structural modifications have been made resulting in markedly active chemical congeners, which were designed, synthetized and tested pharmacologically.
测定了新合成的吡嗪咪唑啉对离体大鼠尾动脉收缩、大鼠心房变时作用的影响以及对麻醉大鼠血压的影响。研究了包括标准咪唑啉药物在内的构效关系。从实际无活性的衍生物开始，逐步进行结构修饰，得到了活性显著的化学同系物，对其进行了设计、合成及药理测试。
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