Synthesis and Positive Inotropic Evaluation of (E)‐2‐(4‐Cinnamylpiperazin‐1‐yl)‐N‐(1‐substituted‐4,5‐dihydro‐[1,2,4]triazolo[4,3‐a]quinolin‐7‐yl)acetamides |
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| Authors: | Yan Wu Long‐Xu Ma Tian‐Wei Niu Fan‐Ling Meng Xun Cui Hu‐Ri Piao |
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| Affiliation: | 1. Key Laboratory of Natural Resources and Functional Molecules of the Changbai Mountain, Affiliated Ministry of Education, Yanbian University College of Pharmacy, Yanji, P. R. China;2. Yanbian University College of Medicine, Yanji, P. R. China |
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| Abstract: | A series of (E)‐2‐(4‐cinnamylpiperazin‐1‐yl)‐N‐(1‐substituted‐4,5‐dihydro‐[1,2,4]triazolo[4,3‐a]quinolin‐7‐yl)acetamides were synthesized and evaluated for their positive inotropic activity by measuring the left atrium stroke volume on isolated rabbit heart preparations. This class of compounds presented favorable in vitro activity compared with the standard drug, milrinone, among which N‐(1‐(3‐chlorophenyl)‐4,5‐dihydro‐[1,2,4]triazolo[4,3‐a]quinolin‐7‐yl)‐2‐(4‐cinnamylpiperazin‐1‐yl)acetamide 5e was found to be the most potent with 16.58 ± 0.11% increased stroke volume (milrinone: 2.46 ± 0.07%) at a concentration of 3 × 10?5 M. The chronotropic effects of the compounds having inotropic effects were also evaluated. |
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| Keywords: | 1‐Cinnamylpiperazine Positive inotropic activity Stroke volume [1,2,4]Triazolo[4,3‐a]quinoline |
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