708983-83-9Relevant articles and documents
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
Wu, Yan,Ma, Long-Xu,Niu, Tian-Wei,Cui, Xun,Piao, Hu-Ri
, p. 4229 - 4232 (2012)
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.
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
Liu, Ji-Yong,Yu, Hai-Ling,Quan, Zhe-Shan,Cui, Xun,Piao, Hu-Ri
scheme or table, p. 2392 - 2395 (2009/12/07)
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
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
Li, Jing-Yuan,Cui, Xun,Liu, Xue-Kun,Hong, Lan,Quan, Zhe-Shan,Piao, Hu-Ri
scheme or table, p. 794 - 799 (2009/04/07)
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.