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Volume 29 Issue 5
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Article Navigation >  Journal of Pharmaceutical Practice and Service  > 2011  >  29(5): 362-365

WANG Shu-dong, CHEN Xing-dong, ZHAO Qing-jie, ZOU Yan, HU Hong-gang, YU Shi-chong, WANG Ting, CHAI Xiao-yun, REN Hai-xiang. Synthesis and platelet aggregation inhibition activity of new derivatives of pyridazinone[J]. Journal of Pharmaceutical Practice and Service, 2011, 29(5): 362-365.
Citation: WANG Shu-dong, CHEN Xing-dong, ZHAO Qing-jie, ZOU Yan, HU Hong-gang, YU Shi-chong, WANG Ting, CHAI Xiao-yun, REN Hai-xiang. Synthesis and platelet aggregation inhibition activity of new derivatives of pyridazinone[J]. Journal of Pharmaceutical Practice and Service, 2011, 29(5): 362-365.
shu

Synthesis and platelet aggregation inhibition activity of new derivatives of pyridazinone

  • 1.

    The Nanjing General Hospital of Nanjing Military Command, Nanjing 210002, China

  • 2.

    School of pharmacy, Second Military Medical University, Shanghai, 200433, China

  • Received Date: 2011-05-10
  • Rev Recd Date: 2011-08-26
  • Objective To study the antiplatelet aggregative activity of 6-(4-substitued acetamino-phenyl 4, 5-dihydro-3(2H)-pyridazinones with different substituted secondary amines. Methods Ten target compounds were designed and synthesized.All of them were confirmed by 1H-NMR spectra. Born method was applied for preliminary pharmacological test in vitro. Results All of the target compounds were not reported.The results of preliminary pharmacological test showed that all the target compounds exhibited potent anti-platelet aggregative activity to a certain extent.Compounds 9c, 9f and 9j were better than MCI-154 and CCI-17910 in vitro. Conclution The steric hindrance and hydrophilicity of different substituted secondary amines impact the anti-platelete aggative activity.
  • [1] Bristol JA,Sircar L,Moos WH,et al.Cardiotonic agents. 1. 4, 5-Dihydro-6-[4-(1H-imidazol-1-yl)phenyl]-3(2H)-pyridazinones: novel positive inotropic agents for the treatment of congestive heart failure[J]. J Med Chem, 1984, 27(9): 1099.
    [2] 蒋 勤, 孙常晟.6-(4-取代苯基)-4,5-二氢-3(2H)-哒嗪酮类化合物的合成及其抑制血小板的作用[J]. 药学学报,1990,25(8):598.
    [3] Mikashima H,Nakao T,Goto K.Y-590 (A new pyridazinone derivative), a potent anti-thrombotic agent-I. Effect on platelet function[J]. Thromb Res, 1983,31(4): 599.
    [4] 王恩思,沈家聪.新型强心药匹莫苯的合成[J].中国药物化学杂志,1997,7(3):185.
    [5] Bom GVR.Aggregation of bloodplatelets by adenosine diphosphate and its reversal[J].Nature,1962,194(4832):927.
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  • 1. 

    沈阳化工大学材料科学与工程学院 沈阳 110142

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Synthesis and platelet aggregation inhibition activity of new derivatives of pyridazinone

  • 1. The Nanjing General Hospital of Nanjing Military Command, Nanjing 210002, China
  • 2. School of pharmacy, Second Military Medical University, Shanghai, 200433, China
  • Received Date: 2011-05-10
  • Rev Recd Date: 2011-08-26

Abstract: Objective To study the antiplatelet aggregative activity of 6-(4-substitued acetamino-phenyl 4, 5-dihydro-3(2H)-pyridazinones with different substituted secondary amines. Methods Ten target compounds were designed and synthesized.All of them were confirmed by 1H-NMR spectra. Born method was applied for preliminary pharmacological test in vitro. Results All of the target compounds were not reported.The results of preliminary pharmacological test showed that all the target compounds exhibited potent anti-platelet aggregative activity to a certain extent.Compounds 9c, 9f and 9j were better than MCI-154 and CCI-17910 in vitro. Conclution The steric hindrance and hydrophilicity of different substituted secondary amines impact the anti-platelete aggative activity.

WANG Shu-dong, CHEN Xing-dong, ZHAO Qing-jie, ZOU Yan, HU Hong-gang, YU Shi-chong, WANG Ting, CHAI Xiao-yun, REN Hai-xiang. Synthesis and platelet aggregation inhibition activity of new derivatives of pyridazinone[J]. Journal of Pharmaceutical Practice and Service, 2011, 29(5): 362-365.
Citation: WANG Shu-dong, CHEN Xing-dong, ZHAO Qing-jie, ZOU Yan, HU Hong-gang, YU Shi-chong, WANG Ting, CHAI Xiao-yun, REN Hai-xiang. Synthesis and platelet aggregation inhibition activity of new derivatives of pyridazinone[J]. Journal of Pharmaceutical Practice and Service, 2011, 29(5): 362-365.
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