Synthesis and inotropic evaluation of 1-substituted-N-(4,5-dihydro-1-methyl-[1,2,4]triazolo[4,3-a]quinolin-7-yl)piperidine-4-carboxamides |
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| Authors: | Ji-Yong Liu Hai-Ling Yu Zhe-Shan Quan Xun Cui Hu-Ri Piao |
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| Institution: | 1. Changbai Mountain Key Laboratory of Natural Resources and Functional Molecules, Affiliated Ministry of Education, Yanbian University College of Pharmacy, Yanji 133000, PR China;2. Yanbian University College of Preclinical Medicine, Yanji 133000, PR China |
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| Abstract: | A series of 1-substituted-N-(4,5-dihydro-1-methyl-1,2,4]triazolo4,3-a]quinolin-7-yl) piperidine-4-carboxamides has been synthesized and evaluated for positive inotropic activity by measuring left atrium stroke volume in isolated rabbit-heart preparations. Some of these derivatives exhibited favorable activity compared with the standard drug, milrinone, among which 1-(2-fluorobenzyl)-N-(4,5-dihydro-1-methyl-1,2,4]triazolo4,3-a]quinolin-7-yl)piperidine-4-carboxamide 6a was the most potent, increasing stroke volume by 11.92 ± 0.35% (milrinone: 6.36 ± 0.13%) at 1 × 10?4 M. |
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