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Synthesis and biological evaluation of n-butylphthalide derivatives as anti-platelet aggregation agents

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收录情况： ◇ SCIE

作者：

机构： [1]Guangdong Provincial Acadamy of Chinese Medical Sciences, Guangdong Provincial Hospital of Chinese Medicine, Guangzhou, China [2]School of Pharmaceutical Sciences, Sun Yat-Sen University, Guangzhou, China [3]Longquanyi District Hospital of Traditional Chinese Medicine, Chengdu, China [4]Laboratory Affiliated to National Key Discipline of Orthopaedic and Traumatology of Chinese Medicine, Guangzhou University of Chinese Medicine, Guangzhou, China [5]State Key Laboratory of Oncology in South China, Sun Yat-Sen University Cancer Center, Guangzhou, China

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关键词： n-Butylphthalide analogues water solubility anti-platelet aggregation

摘要：

New analogues of n-butylphthalide (NBP) bearing various lengths of alkyl and different substitution at the two-position of phthalide were designed and synthesised. Preliminary evaluation and prediction of ACD LogP software indicate that the derivatives display significant improvement in water solubility than NBP does. Further biological analysis showed that NBP analogues specifically inhibit platelet aggregation induced by arachidonic acid but have no effect on that induced by adenosine 5-diphosphate. Especially compounds 1 and 3 were stronger than classical anti-platelet drug, aspirin, and equal potent with NBP, respectively. These findings provide an alternative approach to the development of NBP analogues with anti-platelet aggregation activity with good water solubility for the intervention of ischemic stroke. [GRAPHICS] .

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出版当年[2015]版：

大类 | 4 区化学

小类 | 4 区应用化学 4 区药物化学

最新[2025]版：

大类 | 3 区化学

小类 | 3 区应用化学 4 区药物化学

JCR分区：

出版当年[2014]版：

Q3 CHEMISTRY, APPLIED Q4 CHEMISTRY, MEDICINAL

最新[2023]版：

Q3 CHEMISTRY, APPLIED Q3 CHEMISTRY, MEDICINAL

影响因子： 1.9 最新[2023版] 2.1 最新五年平均 0.919 出版当年[2014版] 1.035 出版当年五年平均 1.225 出版前一年[2013版] 1.057 出版后一年[2015版]

第一作者：

第一作者机构： [1]Guangdong Provincial Acadamy of Chinese Medical Sciences, Guangdong Provincial Hospital of Chinese Medicine, Guangzhou, China [4]Laboratory Affiliated to National Key Discipline of Orthopaedic and Traumatology of Chinese Medicine, Guangzhou University of Chinese Medicine, Guangzhou, China

通讯作者：

通讯机构： [1]Guangdong Provincial Acadamy of Chinese Medical Sciences, Guangdong Provincial Hospital of Chinese Medicine, Guangzhou, China [4]Laboratory Affiliated to National Key Discipline of Orthopaedic and Traumatology of Chinese Medicine, Guangzhou University of Chinese Medicine, Guangzhou, China

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