Acetamide

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  • 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.

  • 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.

  • 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
    Bioorganic & Medicinal Chemistry Letters, 2012
    Co-Authors: Tianwei Niu, Xun Cui, Hu-ri Piao
    Abstract:

    Abstract 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 of 2 4 substitutedbenzyl 1 4 diazepan 1 yl n 1 methyl 4 5 dihydro 1 2 4 triazolo 4 3 a quinolin 7 yl Acetamides as inotropic agents
    Chemical Biology & Drug Design, 2011
    Co-Authors: Xuekun Liu, Xun Cui, Shengming Jiang, Hu-ri Piao
    Abstract:

    In an attempt to search for more potent positive inotropic agents, a series of N-(4,5-dihydro-1-methyl-[1,2,4]triazolo[4,3-a]quinolin-7-yl)-2-(substitutedbenzyl-[1,4]diazepan-1-yl)Acetamides were 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 2-(4-(4-methylbenzyl)-[1,4]-diazepan-1-yl)-N-(4,5-dihydro-1-methyl-[1,2,4]triazolo[4,3-a]quinolin-7-yl)Acetamide (6m) was the most potent, increasing stroke volume by 8.38±0.16% (milrinone 2.45± 0.06%) at 3 x 10(-5) m. The chronotropic effects of those compounds having inotropic effects were also evaluated in this work.

  • 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.

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.

  • 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.

  • 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
    Bioorganic & Medicinal Chemistry Letters, 2012
    Co-Authors: Tianwei Niu, Xun Cui, Hu-ri Piao
    Abstract:

    Abstract 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 of 2 4 substitutedbenzyl 1 4 diazepan 1 yl n 1 methyl 4 5 dihydro 1 2 4 triazolo 4 3 a quinolin 7 yl Acetamides as inotropic agents
    Chemical Biology & Drug Design, 2011
    Co-Authors: Xuekun Liu, Xun Cui, Shengming Jiang, Hu-ri Piao
    Abstract:

    In an attempt to search for more potent positive inotropic agents, a series of N-(4,5-dihydro-1-methyl-[1,2,4]triazolo[4,3-a]quinolin-7-yl)-2-(substitutedbenzyl-[1,4]diazepan-1-yl)Acetamides were 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 2-(4-(4-methylbenzyl)-[1,4]-diazepan-1-yl)-N-(4,5-dihydro-1-methyl-[1,2,4]triazolo[4,3-a]quinolin-7-yl)Acetamide (6m) was the most potent, increasing stroke volume by 8.38±0.16% (milrinone 2.45± 0.06%) at 3 x 10(-5) m. The chronotropic effects of those compounds having inotropic effects were also evaluated in this work.

  • 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.

Xuekun Liu - One of the best experts on this subject based on the ideXlab platform.

  • synthesis of 2 4 substitutedbenzyl 1 4 diazepan 1 yl n 1 methyl 4 5 dihydro 1 2 4 triazolo 4 3 a quinolin 7 yl Acetamides as inotropic agents
    Chemical Biology & Drug Design, 2011
    Co-Authors: Xuekun Liu, Xun Cui, Shengming Jiang, Hu-ri Piao
    Abstract:

    In an attempt to search for more potent positive inotropic agents, a series of N-(4,5-dihydro-1-methyl-[1,2,4]triazolo[4,3-a]quinolin-7-yl)-2-(substitutedbenzyl-[1,4]diazepan-1-yl)Acetamides were 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 2-(4-(4-methylbenzyl)-[1,4]-diazepan-1-yl)-N-(4,5-dihydro-1-methyl-[1,2,4]triazolo[4,3-a]quinolin-7-yl)Acetamide (6m) was the most potent, increasing stroke volume by 8.38±0.16% (milrinone 2.45± 0.06%) at 3 x 10(-5) m. The chronotropic effects of those compounds having inotropic effects were also evaluated in this work.

  • 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.

Tianwei Niu - One of the best experts on this subject based on the ideXlab platform.

S. Dev - One of the best experts on this subject based on the ideXlab platform.

  • density and electrical conductance of calcium nitrate tetrahydrate Acetamide melt
    Journal of Chemical & Engineering Data, 1995
    Co-Authors: S. K. Chettri, S. Dev
    Abstract:

    Density and electrical conductance of the calcium nitrate tetrahydrate+Acetamide melt were measured as functions of temperature and mole fraction of Acetamide. On the basis of the additivity of molar volume, an alternative method has been suggested for estimating the densities of high- or low-melting anhydrous inorganic and organic salts using a suitable hydrate melt as solvent. Molar conductance data were analyzed by using the Vogel-Tammann-Fulcher equation. At ambient temperature the specific conductance of molten calcium nitrate tetrahydrate decreases by the addition of Acetamide as was the case with the addition of KNO 3 −