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丹皮酚肟衍生物的设计、合成及抗血小板聚集活性
引用本文:戴卫国,谭鸿舟,顾宏霞,何冰,何黎琴,黄鹏.丹皮酚肟衍生物的设计、合成及抗血小板聚集活性[J].中国药科大学学报,2022,53(5):535-541.
作者姓名:戴卫国  谭鸿舟  顾宏霞  何冰  何黎琴  黄鹏
作者单位:安徽中医药大学药学院,合肥 230012,安徽中医药大学药学院,合肥 230012,皖西卫生职业学院,六安 237005,安徽中医药大学药学院,合肥 230012,安徽中医药大学药学院,合肥 230012,安徽中医药大学药学院,合肥 230012
基金项目:安徽省高校自然科学研究资助项目(No.KJ2020A0957)
摘    要:以丹皮酚为起始原料,经结构修饰得到25个新的丹皮酚肟类衍生物4a ~ 4y,其结构经过高分辨质谱、核磁共振氢谱确证。所合成的目标化合物对二磷酸腺苷(ADP)和胶原诱导的血小板聚集均具有一定的抑制活性,其中化合物4h、4j对两种诱导剂诱导的血小板聚集优于阳性对照药阿司匹林,且化合物4h具有较好的水溶性和类药性,可作为新的抗血小板活性化合物进一步研究。

关 键 词:丹皮酚肟衍生物  合成  水溶性  抗血小板聚集
收稿时间:2022/5/24 0:00:00
修稿时间:2022/9/21 0:00:00

Design, synthesis and anti-platelet aggregation activity of paeonol oxime derivatives
DAI Weiguo,TAN Hongzhou,GU Hongxi,HE Bing,HE Liqin and HUANG Peng.Design, synthesis and anti-platelet aggregation activity of paeonol oxime derivatives[J].Journal of China Pharmaceutical University,2022,53(5):535-541.
Authors:DAI Weiguo  TAN Hongzhou  GU Hongxi  HE Bing  HE Liqin and HUANG Peng
Affiliation:College of Pharmacy, Anhui University of Chinese Medicine, Hefei 230012,College of Pharmacy, Anhui University of Chinese Medicine, Hefei 230012,West Anhui Health Vocational College, Liuan 237005, China,College of Pharmacy, Anhui University of Chinese Medicine, Hefei 230012,College of Pharmacy, Anhui University of Chinese Medicine, Hefei 230012,College of Pharmacy, Anhui University of Chinese Medicine, Hefei 230012
Abstract:In order to afford new antiplatelet agents with higher potency, a series of paeonol oxime derivatives (4a-4y) were designed and synthesized from paeonol.Their structures were confirmed by HRMS, 1H NMR spectra.The anti-platelet aggregation activity of the target compounds was evaluated.The results revealed that most of them had moderate to good anti-platelet aggregation activity.Among them, compound 4h and 4j were the most potent on adenosine diphosphate (ADP)-induced platelet aggregation and collagen-induced platelet aggregation. Furthermore, the target compound 4h not only showed strong antiplatelet aggregation activity, but also exhibited good water-solubility and drug-like properties, which can be used as a new antiplatelet active compound for further research.
Keywords:peaonol oxime derivatives  synthesis  aqueous solubility  anti-platelet aggregation
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