Design, synthesis and anti-platelet aggregation activity of paeonol oxime derivatives

DAI Weiguo; TAN Hongzhou; GU Hongxia; HE Bing; HE Liqin; HUANG Peng

doi:10.11665/j.issn.1000-5048.20220504

Journal of China Pharmaceutical University > 2022 > 53(5): 535-541. > DOI: 10.11665/j.issn.1000-5048.20220504

DAI Weiguo, TAN Hongzhou, GU Hongxia, HE Bing, HE Liqin, HUANG Peng. Design, synthesis and anti-platelet aggregation activity of paeonol oxime derivatives[J]. Journal of China Pharmaceutical University, 2022, 53(5): 535-541. DOI: 10.11665/j.issn.1000-5048.20220504

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Design, synthesis and anti-platelet aggregation activity of paeonol oxime derivatives

1.
College of Pharmacy, Anhui University of Chinese Medicine, Hefei 230012
2.
West Anhui Health Vocational College, Liuan 237005, China

Funds: This study was supported by the Natural Science Research Project for Colleges and Universities in Anhui Province (No.KJ2020A0957)

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Received Date: May 23, 2022
Revised Date: September 20, 2022

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Abstract

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.
- peaonol oxime derivatives,
- synthesis,
- aqueous solubility,
- anti-platelet aggregation

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