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白花前胡丙素的结构修饰研究
引用本文:吴献礼,孔令义,闵知大.白花前胡丙素的结构修饰研究[J].药学学报,2002,37(7):527-534.
作者姓名:吴献礼  孔令义  闵知大
作者单位:中国药科大学天然药物化学教研室,江苏,南京,210038
基金项目:国家自然科学基金 ( 2 9872 0 5 8),高等学校优秀青年教师教学科研奖励计划,江苏省青年科技基金 (BQ96 0 19)资助课题
摘    要:目的对白花前胡丙素[(+)-praeruptorin A]进行结构修饰,寻找活性化合物。方法首先从白花前胡(Peucedanum praeruptorum)根中分离得到白花前胡丙素,从白花前胡丙素出发,用碱水解及各种酰化反应,半合成各种结构修饰产物。结果得到18个(2~19)凯林内酯类化合物,通过IR,1HNMR和MS等方法确定其结构。结论其中14个(5~18)为新化合物,这些新化合物均有不同程度的钙离子拮抗活性,但作用强度均较白花前胡丙素弱。

关 键 词:白花前胡丙素  结构修饰  钙离子拮抗活性
收稿时间:2001-09-27

STUDIES ON STRUCTURE MODIFICATION OF (+)-PRAERUPTORIN A
WU Xian-li,KONG Ling-yi,MIN Zhi-da.STUDIES ON STRUCTURE MODIFICATION OF (+)-PRAERUPTORIN A[J].Acta Pharmaceutica Sinica,2002,37(7):527-534.
Authors:WU Xian-li  KONG Ling-yi  MIN Zhi-da
Institution:Department of Natural Medicinal Chemistry, China Pharmaceutical University, Nanjing 210038, China.
Abstract:AIM: In order to look for new active compounds, the structure of (+)-praeruptorin A is modified. METHODS: (+)-Praeruptorin A was isolated from the root of Peucedanum praeruptorum, basic hydrolysis of (+)-praeruptorin A and acyled reactions of hydrolysis product of (+)-praeruptorin A were carried out. RESULTS: Eighteen compounds were semi-synthesized from (+)-praeruptorin A. CONCLUSION: Fourteen compounds (5-18) among them are new compounds. Preliminary bioactivity assay indicated that the new compounds show calcium antagonist activity, but they are not as strong as (+)-praeruptorin A.
Keywords:(+)-praeruptorin A  structure modification  calcium antagonist
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