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

oleh: Jian Cui, Le’An Hu, Wei Shi, Guozhen Cui, Xumu Zhang, Qing-Wen Zhang

Format: Article
Diterbitkan: MDPI AG 2019-06-01

Deskripsi

Ginkgolides are the major active component of <i>Ginkgo biloba</i> 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 IC<sub>50</sub> values of 5~21 nM.