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

Cui, Jian1; Hu, Le'An1,2,3; Shi, Wei4; Cui, Guozhen4; Zhang, Xumu2,3; Zhang, Qing-Wen1

2019-06

10.3390/molecules24112156

MOLECULES   影响因子和分区

1420-3049

1420-3049

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 similar to 21 nM.

ginkgolide platelet-activating factor receptor inhibitor

SCI

英语

通讯

Research Committee of the University of Macau[MYRG2016-00046-ICMS-QRCM]

Biochemistry & Molecular Biology ; Chemistry

Biochemistry & Molecular Biology ; Chemistry, Multidisciplinary

WOS:000472631000129

MDPI

CHEMISTRY

Web of Science

1.Univ Macau, Inst Chinese Med Sci, State Key Lab Qual Res Chinese Med, Macau 999078, Peoples R China
2.Southern Univ Sci & Technol, Dept Chem, Shenzhen 518000, Peoples R China
3.Southern Univ Sci & Technol, Shenzhen Grubbs Inst, Shenzhen 518000, Peoples R China
4.Zunyi Med Univ, Dept Bioengn, Zhuhai Campus, Zhuhai 519041, Guangdong, Peoples R China

Cui, Jian,Hu, Le'An,Shi, Wei,et al. Design, Synthesis and Anti-Platelet Aggregation Activity Study of Ginkgolide-1,2,3-triazole Derivatives[J]. MOLECULES,2019,24(11).

Cui, Jian,Hu, Le'An,Shi, Wei,Cui, Guozhen,Zhang, Xumu,&Zhang, Qing-Wen.(2019).Design, Synthesis and Anti-Platelet Aggregation Activity Study of Ginkgolide-1,2,3-triazole Derivatives.MOLECULES,24(11).

Cui, Jian,et al."Design, Synthesis and Anti-Platelet Aggregation Activity Study of Ginkgolide-1,2,3-triazole Derivatives".MOLECULES 24.11(2019).