Kaliszan R, Foks H, Damasiewicz B, Nasal A, Radwańska A, Kuźmierkiewicz W, Pancechowska-Ksepko D, Rudnicka W, Wisterowicz K
Pol J Pharmacol Pharm. 1985 Jan-Feb;37(1):79-88.
A group of new pyrazinylimidazolines was prepared and their effect on the contraction of isolated rat tail artery as well as their effect on blood pressure in urethane anesthetized normotensive rats were tested. The biological responses were compared to those elicited by standard imidazoline drugs and structure-activity relationships were analysed. The new chemical derivatives were subsequently synthetized and tested pharmacologically. Basing on the experimental results obtained and comparing these to the reported data on arylimidazolines the following suggestions have been put forward concerning the further modifications of alpha-adrenergically active pyrazinylimidazolines: 1) a distance of about 5 A should separate imidazoline nitrogen and pyrazine nucleus, 2) bond refractivity of the separating bridge should be above 5.33, 3) hydrophobicity of substituents in pyrazine ring must be possibly high.
制备了一组新型吡嗪基咪唑啉，并测试了它们对离体大鼠尾动脉收缩的影响以及对氨基甲酸乙酯麻醉的正常血压大鼠血压的影响。将这些生物学反应与标准咪唑啉药物引起的反应进行比较，并分析构效关系。随后合成了新的化学衍生物并进行了药理测试。根据获得的实验结果并将其与报道的芳基咪唑啉数据进行比较，对α-肾上腺素能活性吡嗪基咪唑啉的进一步修饰提出了以下建议：1）咪唑啉氮原子与吡嗪核之间应相隔约5埃的距离；2）分隔桥的键折射度应高于5.33；3）吡嗪环中取代基的疏水性必须尽可能高。
