Synthesis and biological evaluation of n-butylphthalide derivatives as anti-platelet aggregation agents |
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| Authors: | Meihui Chen Qi Liu Min Tan Shijun Wen |
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| Institution: | 1. Guangdong Provincial Acadamy of Chinese Medical Sciences, Guangdong Provincial Hospital of Chinese Medicine, Guangzhou, China;2. Laboratory Affiliated to National Key Discipline of Orthopaedic and Traumatology of Chinese Medicine, Guangzhou University of Chinese Medicine, Guangzhou, China;3. School of Pharmaceutical Sciences, Sun Yat-Sen University, Guangzhou, China;4. Longquanyi District Hospital of Traditional Chinese Medicine, Chengdu, China;5. State Key Laboratory of Oncology in South China, Sun Yat-Sen University Cancer Center, Guangzhou, China |
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| Abstract: | 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. |
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| Keywords: | n-Butylphthalide analogues water solubility anti-platelet aggregation |
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