- Synthesis and positive inotropic evaluation of N-(1-oxo-1,2,4,5-tetrahydro- [1,2,4]triazolo[4,3-a]quinolin-7-yl)acetamides bearing piperazine and 1,4-diazepane moieties
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Two series of N-(1-oxo-1,2,4,5-tetrahydro-[1,2,4]triazolo[4,3-a]quinolin-7- yl)acetamides bearing piperazine and 1,4-diazepane moieties were synthesized and screened for their positive inotropic activity by measuring left atrium stroke volume on isolated rabbit heart preparations. Most of the derivatives exhibited better in vitro positive inotropic activity than the existing drug, milrinone, among which 2-(4-(4-chlorobenzyl)-1,4-diazepan-1-yl)-N-(1-oxo-1,2,4,5- tetrahydro-[1,2,4]triazolo[4,3-a]quinolin-7-yl)acetamide 6c proved to be the most potent with 15.48 ± 0.27% increased stroke volume (milrinone: 2.46 ± 0.07%) at a concentration of 3 × 10-5 M. The chronotropic effects of the compounds that exhibited inotropic effects were also evaluated.
- Wu, Yan,Ma, Long-Xu,Niu, Tian-Wei,Cui, Xun,Piao, Hu-Ri
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- Synthesis of new triazole acetamides with inotropic effects
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A series of new triazole acetamides 5a-w were synthesized and evaluated for their positive inotropic activity of left atrium stroke volume on isolated rabbit-heart preparations. The majority of the derivatives presented favorable in vitro activity compared with the reference drug, milrinone. Among them triazole acetamide 5a was identified as the most potent with 20.29 ± 0.18% 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.
- Wu, Yan,Ma, Long-Xu,Sun, Liang-Peng,Song, Ming-Xia,Cui, Xun,Piao, Hu-Ri
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p. 757 - 760
(2013/02/23)
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- 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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A series of 1-substituted-N-(4,5-dihydro-1-methyl-[1,2,4]triazolo[4,3-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 preparation
- Liu, Ji-Yong,Yu, Hai-Ling,Quan, Zhe-Shan,Cui, Xun,Piao, Hu-Ri
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p. 2392 - 2395
(2009/12/07)
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- Synthesis and positive inotropic activity of N-(4,5-dihydro-[1,2,4]triazolo[4,3-a]quinolin-7-yl)-2-(piperazin-1-yl)ac etamide derivatives
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A series of N-(4,5-dihydro-[1,2,4]triazolo[4,3-a]quinolin-7-yl)-2-(piperazin-1-yl)ac etamide derivatives were synthesized and their positive inotropic activity was evaluated by measuring left atrium stroke volume on isolated rabbit heart preparations. Several compounds showed favorable activity compared with the standard drug, milrinone, among which N-(1-benzyl-4,5-dihydro-[1,2,4]triazolo[4,3-a]quinolin-7-yl)-2-(4-benzyl piperazin-1-yl)acetamide 6j was found to be the most potent with the 13.2% increased stroke volume (milrinone 4.7%) at concentration of 3 × 10-5 M in our in vitro study. The chronotropic effects of those compounds having inotropic effects were also evaluated in this work.
- Zhang, Chun-Bo,Cui, Xun,Hong, Lan,Quan, Zhe-Shan,Piao, Hu-Ri
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scheme or table
p. 4606 - 4609
(2009/04/06)
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- Synthesis and positive inotropic evaluation of 2-(4-(4-substituted benzyloxy)-3-methoxybenzyl)-1,4-diazepan-1-yl-n-(4,5-dihydro-1-methyl[1,2,4] triazolo[4,3-a]quinolin-7-yl)-acetamides
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In an attempt to search for more potent positive inotropic agents, a series of 2-(4-(4-substituted benzyloxy)-3-methoxybenzyl)-1,4-diazepan-1-yl)-N-(4,5- dihydro-1-methyl[1,2,4]triazolo[4,3-a]quinolin-7-yl)acetamides was synthesized and their positive inotropic activities were evaluated by measuring left atrium stroke volume on isolated rabbit-heart preparations. Several compounds showed favorable activity compared with the standard drug Milrinone among which 2-(4-(4-(2-chlorobenzyloxy)-3-methoxybenzyl)-1,4-diazepan-1-yl)-N-(4, 5-dihydro-1-methyl-[1,2,4]triazolo[4,3-a]quinolin-7-yl)acetamide 6e was found to have the most desirable potency with the 6.79 ± 0.18% increased stroke volume (Milrinone: 1.67 ± 0.64%) at a concentration of 1 × 10 -5 M in our in-vitro study. The chronotropic effects of those compounds having inotropic effects were also evaluated in this work.
- Li, Jing-Yuan,Cui, Xun,Liu, Xue-Kun,Hong, Lan,Quan, Zhe-Shan,Piao, Hu-Ri
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scheme or table
p. 794 - 799
(2009/04/07)
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