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Open AccessArticle

Design, Synthesis and Anti-Platelet Aggregation Activity Study of Ginkgolide-1,2,3-triazole Derivatives

1
State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau, Macau 999078, China
2
Department of Chemistry and Shenzhen Grubbs Institute, Southern University of Science and Technology, Shenzhen 518000, China
3
Department of Bioengineering, Zhuhai Campus of Zunyi Medical University, Zhuhai 519041, Guangdong, China
*
Authors to whom correspondence should be addressed.
These authors contributed equally to the work.
Molecules 2019, 24(11), 2156; https://doi.org/10.3390/molecules24112156
Received: 7 May 2019 / Revised: 27 May 2019 / Accepted: 3 June 2019 / Published: 7 June 2019
(This article belongs to the Special Issue Synthesis, Study and Utilization of Natural Products)
Ginkgolides are the major active component of Ginkgo biloba for inhibition of platelet activating factor receptor. An azide-alkyne Huisgen cycloaddition reaction was used to introduce a triazole nucleus into the target ginkgolide molecules. A series of ginkgolide-1,2,3-triazole conjugates with varied functional groups including benzyl, phenyl and heterocycle moieties was thus synthesized. Many of the designed derivatives showed potent antiplatelet aggregation activities with IC50 values of 5~21 nM. View Full-Text
Keywords: ginkgolide; platelet-activating factor receptor; inhibitor ginkgolide; platelet-activating factor receptor; inhibitor
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MDPI and ACS Style

Cui, J.; Hu, L.; Shi, W.; Cui, G.; Zhang, X.; Zhang, Q.-W. Design, Synthesis and Anti-Platelet Aggregation Activity Study of Ginkgolide-1,2,3-triazole Derivatives. Molecules 2019, 24, 2156.

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