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首页> 外文期刊>Medicinal chemistry >Synthesis of 2-(4-substitutedbenzylpiperazin-1-yl)-N-(2-oxo-2,3- dihydrobenzooxazol- 6-yl)acetamides as inotropic agents
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Synthesis of 2-(4-substitutedbenzylpiperazin-1-yl)-N-(2-oxo-2,3- dihydrobenzooxazol- 6-yl)acetamides as inotropic agents

机译:以正离子剂的形式合成2-(4-取代的苄基哌嗪-1-基)-N-(2-氧代-2,3-二氢苯并恶唑-6-基)乙酰胺

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摘要

We describe the synthesis and positive inotropic evaluation of a series of 2-(4-substitutedbenzylpiperazin-1-yl)- N-(2-oxo-2,3-dihydrobenzooxazol-6-yl) acetamides by measuring left atrial stroke volume in preparations of isolated rabbit hearts. Several compounds were developed from and showed favorable activities compared with the standard drug milrinone. Compound 4l was the most potent with an increased stroke volume of 11.78 ± 0.18% (milrinone 6.36 ± 0.13%) at 1 × 10 -4 M in our in-vitro study. The chronotropic effects of compounds having inotropic effects were also evaluated.
机译:我们通过测量制剂中的左心房搏动量来描述一系列2-(4-取代的苄基哌嗪-1-基)-N-(2-氧代-2,3-二氢苯并恶唑-6-基)乙酰胺的合成和正性肌力评估孤立的兔子心。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。在我们的体外研究中,化合物4l最有效,在1×10 -4 M时卒中量增加了11.78±0.18%(米力农6.36±0.13%)。还评估了具有变力作用的化合物的变时作用。

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