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10-O-二烷基氨基乙基银杏内酯B作为血小板活化因子拮抗剂的合成及生物学评价

The synthesis and biological evaluation of 10-O-dialkylaminoethyl ginkgolide B as platelet-activating factor antagonist.

作者信息

Guo Chun-Jun, Ren Yi, Qin Yin-Lin, Zhang Qian

机构信息

Department of Medicinal Chemistry, School of Pharmacy, Fudan University, Shanghai, China.

出版信息

J Asian Nat Prod Res. 2008 Sep-Oct;10(9-10):989-92. doi: 10.1080/10286020802240376.

Abstract

Four nitrogen-containing derivatives of ginkgolide B were synthesized to improve the physical-chemical properties and bioavailability of ginkgolide B. The reaction was accomplished with the nitrogen atom as neighboring group participating in the replacement reaction. All of the four compounds were proved to have excellent inhibiting effect on rabbit platelet aggregation induced by platelet-activating factor which is as well as ginkgolide B.

摘要

合成了银杏内酯B的四种含氮衍生物,以改善银杏内酯B的物理化学性质和生物利用度。该反应通过氮原子作为邻基参与取代反应来完成。已证明这四种化合物对血小板活化因子诱导的兔血小板聚集均具有优异的抑制作用,其作用与银杏内酯B相当。

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