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Medicinal Chemistry

Editor-in-Chief

ISSN (Print): 1573-4064
ISSN (Online): 1875-6638

Synthesis of 2-(4-substitutedbenzylpiperazin-1-yl)-N-(2-oxo-2,3-dihydrobenzooxazol- 6-yl)acetamides as Inotropic Agents

Author(s): Tianyi Zhang, Liangpeng Sun, Xuekun Liu, Xun Cui and Huri Piao

Volume 8, Issue 6, 2012

Page: [1093 - 1098] Pages: 6

DOI: 10.2174/1573406411208061093

Price: $65

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


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