Abstract
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.
Keywords: 2, 3-Dihydro-2-oxobenzo[d]oxazole, Positive inotropic activity, Stroke volume
Medicinal Chemistry
Title:Synthesis of 2-(4-substitutedbenzylpiperazin-1-yl)-N-(2-oxo-2,3-dihydrobenzooxazol- 6-yl)acetamides as Inotropic Agents
Volume: 8 Issue: 6
Author(s): Tianyi Zhang, Liangpeng Sun, Xuekun Liu, Xun Cui and Huri Piao
Affiliation:
Keywords: 2, 3-Dihydro-2-oxobenzo[d]oxazole, Positive inotropic activity, Stroke volume
Abstract: 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.
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Cite this article as:
Zhang Tianyi, Sun Liangpeng, Liu Xuekun, Cui Xun and Piao Huri, Synthesis of 2-(4-substitutedbenzylpiperazin-1-yl)-N-(2-oxo-2,3-dihydrobenzooxazol- 6-yl)acetamides as Inotropic Agents, Medicinal Chemistry 2012; 8 (6) . https://dx.doi.org/10.2174/1573406411208061093
DOI https://dx.doi.org/10.2174/1573406411208061093 |
Print ISSN 1573-4064 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6638 |
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