Abstract
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.
Highlights
Ginkgo biloba, named maidenhair tree, the only surviving species from the family Ginkgoaceae has existed for more than 180 million years, and for this reason it was called a “living fossil” by Darwin.G. biloba has been used as a traditional Chinese medicine for a long time for the treatment of lung weakness, asthma, coughing, cancer, etc [1,2]
1965, when a German company developed from ginkgo extracts a botanical medicine named EGB761, with various effects on central nervous system (CNS) diseases, including Alzheimer’s disease, dementia, hypomnesia, etc [3,4]
From the results shown above, we can preliminarily conclude that non-substituted benzyl and phenyl 1,2,3-triazole conjugates have significantly enhanced antiplatelet aggregation activities compared to ginkgolide B (1)
Summary
Named maidenhair tree, the only surviving species from the family Ginkgoaceae has existed for more than 180 million years, and for this reason it was called a “living fossil” by Darwin. It’s noteworthy that the introduction of bulky or aromatic or aromatic substituents at 10-OH could help to increase activity against PAFR [17,18]. A series of ginkgolide derivatives with 1,2,3-triazole moieties connected with various benzyl, phenyl and heterocycle moieties at the C-10 position were designed and synthetized. Various benzyl, phenyl and heterocycle moieties at the C-10 position were designed and synthetized Their antiplatelet aggregation activities were evaluated and several derivatives displayed more potent inhibitory effects against PAFR than the natural ginkgolide B, with IC values of 5~21 nM, potent inhibitory effects against PAFR than the natural ginkgolide B, with IC50 50 values of 5~21 nM, or or about 10 to 20 times higher than the natural compound.
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