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:Yanbian University College of Pharmacy, Yanji City, Jilin Province 133000, P.R. China.
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.
