Synthesis and pharmacological evaluation of new 1-(3-(4-arylpiperazin-1-yl)-2-hydroxypropyl)-pyrrolidin-2-one derivatives with anti-arrhythmic, hypotensive, and alpha-adrenolytic activity.

Kulig K; Sapa J; Maciag D; Filipek B; Malawska B

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Synthesis and pharmacological evaluation of new 1-(3-(4-arylpiperazin-1-yl)-2-hydroxypropyl)-pyrrolidin-2-one derivatives with anti-arrhythmic, hypotensive, and alpha-adrenolytic activity.

机译：具有抗心律不齐，降压和α-肾上腺素分解活性的新型1-（3-（4-（4-芳基哌嗪-1-基）-2-羟丙基）-吡咯烷-2-酮衍生物的合成和药理评估。

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A series of novel arylpiperazines bearing a pyrrolidin-2-one fragment was synthesized and evaluated for the binding affinity of the alpha(1)- and alpha(2)-adrenoceptors (AR) and for the antiarrhythmic and hypotensive activities of the compounds. The most potent and selective compound 1-[2-hydroxy-3-[4-[(2-hydroxyphenyl)piperazin-1-yl]propyl]pyrrolidin-2-one 8 binds with pK(i) = 6.71 for alpha(1)-AR. Derivative 8 was also the most active in the prophylactic antiarrhythmic test in adrenaline-induced arrhythmia in anaesthetized rats. Its ED(50 )value equals 1.9 mg/kg (i.v.). Compounds with substituents such as a fluorine atom 4, a methyl 5, or a hydroxyl 8 group, or two substituents such as fluorine/chlorine atoms and methoxy groups in the phenyl ring, significantly decreased the systolic and diastolic pressure in normotensive anesthetized rats at a dosages of 5-10 mg/kg (i.v.). It was found that the presence of the piperazine ring and a hydroxy group in the second position of the propyl chain are critical structural features in determining the affinity of the compounds tested.

机译：合成了一系列带有吡咯烷基-2-酮片段的新型芳基哌嗪，并对其α（1）-和α（2）-肾上腺素能受体（AR）的结合亲和力以及该化合物的抗心律不齐和降压活性进行了评估。最有效和选择性最大的化合物1- [2-羟基-3- [4-[（（2-羟基苯基）哌嗪-1-基]丙基]吡咯烷酮-2-酮8与pK（i）= 6.71结合成alpha（1 ）-AR。在麻醉大鼠中，在肾上腺素诱发的心律失常的预防性抗心律失常测试中，衍生物8也是最活跃的。 ED（50）值等于1.9 mg / kg（i.v.）。具有取代基（例如氟原子4，甲基5或羟基8）或两个取代基（例如苯环中的氟/氯原子和甲氧基）的化合物可显着降低常压麻醉大鼠的收缩压和舒张压。剂量为5-10 mg / kg（iv）。已经发现，在丙基链的第二位的哌嗪环和羟基的存在是确定测试化合物的亲和力的关键结构特征。

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《Archiv der Pharmazie》 |2007年第9期|共10页
作者
Kulig K; Sapa J; Maciag D; Filipek B; Malawska B;
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正文语种 eng
中图分类药学;
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Animals; Anti-Arrhythmia Agents; Antihypertensive Agents; Blood Pressure; 动物; 抗心律失常药; 抗高血压药; 血压; 药物相互作用; 模型; 分子; 吡咯烷酮类;

机译：Animals;Anti-Arrhythmia Agents;Antihypertensive Agents;Blood Pressure;动物;抗心律失常药;抗高血压药;血压;药物相互作用;模型;分子;吡咯烷酮类;

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机译：具有抗心律不齐，降压和α-肾上腺素分解活性的新型1-（3-（4-（4-芳基哌嗪-1-基）-2-羟丙基）-吡咯烷-2-酮衍生物的合成和药理评估。
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Synthesis and pharmacological evaluation of new 1-(3-(4-arylpiperazin-1-yl)-2-hydroxypropyl)-pyrrolidin-2-one derivatives with anti-arrhythmic, hypotensive, and alpha-adrenolytic activity.

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