Synthesis and Positive Inotropic Activity of [1,2,4]Triazolo[4,3-a] Quinoxaline Derivatives Bearing Substituted Benzylpiperazine and Benzoylpiperazine Moieties

Xue‐Kun Liu, Long-xu Ma, Zhi-Yu Wei, X. Cui, Shi Zhan, Xiumei Yin, H. Piao
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引用次数: 3

Abstract

In an attempt to search for more potent positive inotropic agents, two series of [1,2,4]triazolo[4,3-a] quinoxaline derivatives bearing substituted benzylpiperazine and benzoylpiperazine moieties were synthesized and their positive inotropic activities evaluated by measuring left atrial stroke volume in isolated rabbit heart preparations. Several compounds showed favorable activities compared with the standard drug, milrinone. Compound 6c was the most potent agent, with an increased stroke volume of 12.53% ± 0.30% (milrinone: 2.46% ± 0.07%) at 3 × 10−5 M. The chronotropic effects of compounds having considerable inotropic effects were also evaluated.
含取代苯甲酰哌嗪和苯甲酰哌嗪的[1,2,4]三唑[4,3-a]喹诺啉衍生物的合成及正性正性活性研究
为了寻找更有效的正性肌力药物,我们合成了两个系列的三唑[1,2,4]喹诺啉衍生物,它们含有取代的苯甲酰哌嗪和苯甲酰哌嗪基团,并通过测量离体兔心脏制剂的左心房卒中容积来评估它们的正性肌力活性。与标准药物米立酮相比,几种化合物表现出良好的活性。化合物6c是最有效的药物,在3 × 10−5 m时可使脑卒中体积增加12.53%±0.30%(米立酮:2.46%±0.07%)。
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