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Synthesis and positive inotropic evaluation of [1,2,4]triazolo[3,4-a]phthalazine and tetrazolo[5,1-a]phthalazine derivatives bearing substituted piperazine moieties
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2014-03-03 , DOI: 10.1016/j.bmcl.2014.02.040 Long-Xu Ma , Bai-Ri Cui , Yan Wu , Jia-Chun Liu , Xun Cui , Li-Ping Liu , Hu-Ri Piao
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2014-03-03 , DOI: 10.1016/j.bmcl.2014.02.040 Long-Xu Ma , Bai-Ri Cui , Yan Wu , Jia-Chun Liu , Xun Cui , Li-Ping Liu , Hu-Ri Piao
Four series of [1,2,4]triazolo[3,4-]phthalazine and tetrazolo[5,1-]phthalazine derivatives bearing substituted piperazine moieties were synthesized and evaluated for their positive inotropic activity by measuring the left atrium stroke volume in isolated rabbit-heart preparations. Several compounds were developed and showed favorable activities compared to the standard drug milrinone, with (4-([1,2,4]triazolo[3,4-]phthalazin-6-yl)piperazin-1-yl)(-tolyl)methanone () being identified as the most potent with an increased stroke volume of 19.15±0.22% (milrinone: 2.46±0.07%) at a concentration of 3×10M. A preliminary study of mechanism of action revealed that displayed its positive inotropic effect may be related to the PDE-cAMP-PKA signaling pathway. Compounds exhibiting inotropic effects were also evaluated in terms of the chronotropic effects.
中文翻译:
带有取代哌嗪部分的[1,2,4]三唑并[3,4-a]酞嗪和四唑并[5,1-a]酞嗪衍生物的合成和正性肌力评价
合成了四个系列的带有取代哌嗪部分的[1,2,4]三唑并[3,4-]酞嗪和四唑并[5,1-]酞嗪衍生物,并通过测量分离的左心房搏出量来评估其正性肌力活性。兔心制剂。与标准药物米力农相比,开发了几种化合物,并显示出良好的活性,其中(4-([1,2,4]三唑并[3,4-]酞嗪-6-基)哌嗪-1-基)(-甲苯基)甲酮 () 被认为是最有效的,浓度为 3×10M 时每搏输出量增加 19.15±0.22%(米力农:2.46±0.07%)。作用机制初步研究表明其正性肌力作用可能与PDE-cAMP-PKA信号通路有关。还根据变时作用评价表现出正性肌力作用的化合物。
更新日期:2014-03-03
中文翻译:
![](https://scdn.x-mol.com/jcss/images/paperTranslation.png)
带有取代哌嗪部分的[1,2,4]三唑并[3,4-a]酞嗪和四唑并[5,1-a]酞嗪衍生物的合成和正性肌力评价
合成了四个系列的带有取代哌嗪部分的[1,2,4]三唑并[3,4-]酞嗪和四唑并[5,1-]酞嗪衍生物,并通过测量分离的左心房搏出量来评估其正性肌力活性。兔心制剂。与标准药物米力农相比,开发了几种化合物,并显示出良好的活性,其中(4-([1,2,4]三唑并[3,4-]酞嗪-6-基)哌嗪-1-基)(-甲苯基)甲酮 () 被认为是最有效的,浓度为 3×10M 时每搏输出量增加 19.15±0.22%(米力农:2.46±0.07%)。作用机制初步研究表明其正性肌力作用可能与PDE-cAMP-PKA信号通路有关。还根据变时作用评价表现出正性肌力作用的化合物。