Synthesis and platelet aggregation inhibition activity of new derivatives of pyridazinone

SONG Yan; CANG Jie; MENG Lei; MA Fujia

doi:10.3969/j.issn.1006-0111.2014.02.008

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Objective To study the antiplatelet aggregative activity of 6-(4-substitued acetamino-phenyl 4,5-dihydro-3(2H)-pyridazinones with different amino group. Methods Nine 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 antiplatelet aggregative activity to a certain extent.Compounds 9c, 9e and 9i were better than MCI-154 and CCI-17910 in vitro. Conclusion Inletting different substituted amino groups could enhance the antiplatelet aggregation activity of the compounds.

Synthesis and platelet aggregation inhibition activity of new derivatives of pyridazinone

No. 455 Hospital of PLA, Shanghai 200052, China

Received Date: 2013-06-11

Rev Recd Date: 2013-10-16

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Abstract: Objective To study the antiplatelet aggregative activity of 6-(4-substitued acetamino-phenyl 4,5-dihydro-3(2H)-pyridazinones with different amino group. Methods Nine 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 antiplatelet aggregative activity to a certain extent.Compounds 9c, 9e and 9i were better than MCI-154 and CCI-17910 in vitro. Conclusion Inletting different substituted amino groups could enhance the antiplatelet aggregation activity of the compounds.

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Reference (7)

[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]	Yang GM, Liu LM, Xu J. Effects of MIC-154 on vascular reactivity and its mechanisms after hemorrhggic shock in rats[J].J Cardiovasc Pharmacol, 2006, 47(6):751.
[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]	王曙东, 陈兴东, 赵庆杰, 等. 哒嗪酮类新衍生物的合成及其对血小板聚集的抑制作用[J].药学实践杂志, 2011,29(5):362.
[5]	章杰兵, 柴晓云, 俞世冲, 等. 哒嗪酮类新衍生物的合成及其对血小板聚集的抑制作用[J].第二军医大学学报, 2009,30(7):821.
[6]	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.
[7]	Bom GVR.Aggregation of bloodplatelets by adenosine diphosphate and its reversal[J].Nature,1962,194(4832):927.

[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]	Yang GM, Liu LM, Xu J. Effects of MIC-154 on vascular reactivity and its mechanisms after hemorrhggic shock in rats[J].J Cardiovasc Pharmacol, 2006, 47(6):751.
[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]	王曙东, 陈兴东, 赵庆杰, 等. 哒嗪酮类新衍生物的合成及其对血小板聚集的抑制作用[J].药学实践杂志, 2011,29(5):362.
[5]	章杰兵, 柴晓云, 俞世冲, 等. 哒嗪酮类新衍生物的合成及其对血小板聚集的抑制作用[J].第二军医大学学报, 2009,30(7):821.
[6]	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.
[7]	Bom GVR.Aggregation of bloodplatelets by adenosine diphosphate and its reversal[J].Nature,1962,194(4832):927.

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Synthesis and platelet aggregation inhibition activity of new derivatives of pyridazinone

doi: 10.3969/j.issn.1006-0111.2014.02.008

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