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Hu-ri Piao – One of the best experts on this subject based on the ideXlab platform.

  • Synthesis of new triazole Acetamides with inotropic effects.
    Bioorganic & medicinal chemistry letters, 2012
    Co-Authors: Liang-peng Sun, Ming-xia Song, Xun Cui, Hu-ri Piao

    Abstract:

    Abstract 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.

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  • 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
    Archiv Der Pharmazie, 2012
    Co-Authors: Tianwei Niu, Xun Cui, Fanling Meng, Hu-ri Piao

    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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  • 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
    Archiv Der Pharmazie, 2008
    Co-Authors: Xun Cui, Xuekun Liu, Lan Hong, Zheshan Quan, Hu-ri Piao

    Abstract:

    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 x 10(-5) M in our in-vitro study. The chronotropic effects of those compounds having inotropic effects were also evaluated in this work.

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Xun Cui – One of the best experts on this subject based on the ideXlab platform.

  • Synthesis of new triazole Acetamides with inotropic effects.
    Bioorganic & medicinal chemistry letters, 2012
    Co-Authors: Liang-peng Sun, Ming-xia Song, Xun Cui, Hu-ri Piao

    Abstract:

    Abstract 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.

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  • 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
    Archiv Der Pharmazie, 2012
    Co-Authors: Tianwei Niu, Xun Cui, Fanling Meng, Hu-ri Piao

    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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  • 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
    Archiv Der Pharmazie, 2008
    Co-Authors: Xun Cui, Xuekun Liu, Lan Hong, Zheshan Quan, Hu-ri Piao

    Abstract:

    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 x 10(-5) M in our in-vitro study. The chronotropic effects of those compounds having inotropic effects were also evaluated in this work.

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Shikai Tian – One of the best experts on this subject based on the ideXlab platform.

  • copper catalyzed oxidative carbamoylation of n arylacrylamides with hydrazinecarboxamides leading to 2 oxindol 3 yl Acetamides
    Advanced Synthesis & Catalysis, 2018
    Co-Authors: Zengyang He, Shikai Tian

    Abstract:

    A tandem radical carbamoylation/cyclization reaction of N-arylacrylamides with hydrazinecarboxamides has been developed for facile access to 2-(oxindol-3-yl)Acetamides, which had been utilized as precursors in the synthesis of natural bioactive pyrrolidinoindolines. In the presence of 1 mol% of copper(II) carbonate and 4 equiv. of tert-butyl hydroperoxide, a wide range of N-arylacrylamides underwent highly regioselective carbamoylation with hydrazinecarboxamides followed by 5-exo-trig cyclization to afford structurally diverse 2-(oxindol-3-yl)Acetamides in moderate to excellent yields.

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  • Copper‐Catalyzed Oxidative Carbamoylation of N‐Arylacrylamides with Hydrazinecarboxamides Leading to 2‐(Oxindol‐3‐yl)Acetamides
    Advanced Synthesis & Catalysis, 2018
    Co-Authors: Zengyang He, Shikai Tian

    Abstract:

    A tandem radical carbamoylation/cyclization reaction of N-arylacrylamides with hydrazinecarboxamides has been developed for facile access to 2-(oxindol-3-yl)Acetamides, which had been utilized as precursors in the synthesis of natural bioactive pyrrolidinoindolines. In the presence of 1 mol% of copper(II) carbonate and 4 equiv. of tert-butyl hydroperoxide, a wide range of N-arylacrylamides underwent highly regioselective carbamoylation with hydrazinecarboxamides followed by 5-exo-trig cyclization to afford structurally diverse 2-(oxindol-3-yl)Acetamides in moderate to excellent yields.

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