云南师范大学学报(自然科学版)
雲南師範大學學報(自然科學版)
운남사범대학학보(자연과학판)
JOURNAL OF YUNAN NORMAL UNIVERSITY(NATURAL SCIENCES EDITION)
2014年
6期
62-68
,共7页
李俊鹏%杨涵%陈家林%周利民%崔浩%陈立桥
李俊鵬%楊涵%陳傢林%週利民%崔浩%陳立橋
리준붕%양함%진가림%주이민%최호%진립교
丹参素%药物合成%不对称催化%构效关系
丹參素%藥物閤成%不對稱催化%構效關繫
단삼소%약물합성%불대칭최화%구효관계
Danshensu%Drug synthesis%Asymmetrical catalysis%SAR
中药丹参的活性成分丹参素是一种化学结构简单但特殊,并具有广泛的生理药理学活性的有机小分子化合物,丹参素类药物在抗心肌缺血和保肝护肝等方面疗效显著。然而,仅依靠从丹参中分离得到丹参素(或其衍生物)远不能满足临床需要。依靠化学方法简洁、高效的合成丹参素(或其衍生物)是该类药物研发亟须解决的问题之一。综述了近年来国内外相关报道,对外消旋体和光学纯丹参素的合成路线进行讨论,并就其构效关系进行初步分析;其中,光学纯丹参素的简单、高效、高选择性合成仍然是药物化学和有机化学关注的重点。新的合成方法和有关丹参素详细的构效关系研究,对开发丹参素类药物具有重要意义。
中藥丹參的活性成分丹參素是一種化學結構簡單但特殊,併具有廣汎的生理藥理學活性的有機小分子化閤物,丹參素類藥物在抗心肌缺血和保肝護肝等方麵療效顯著。然而,僅依靠從丹參中分離得到丹參素(或其衍生物)遠不能滿足臨床需要。依靠化學方法簡潔、高效的閤成丹參素(或其衍生物)是該類藥物研髮亟鬚解決的問題之一。綜述瞭近年來國內外相關報道,對外消鏇體和光學純丹參素的閤成路線進行討論,併就其構效關繫進行初步分析;其中,光學純丹參素的簡單、高效、高選擇性閤成仍然是藥物化學和有機化學關註的重點。新的閤成方法和有關丹參素詳細的構效關繫研究,對開髮丹參素類藥物具有重要意義。
중약단삼적활성성분단삼소시일충화학결구간단단특수,병구유엄범적생리약이학활성적유궤소분자화합물,단삼소류약물재항심기결혈화보간호간등방면료효현저。연이,부의고종단삼중분리득도단삼소(혹기연생물)원불능만족림상수요。의고화학방법간길、고효적합성단삼소(혹기연생물)시해류약물연발극수해결적문제지일。종술료근년래국내외상관보도,대외소선체화광학순단삼소적합성로선진행토론,병취기구효관계진행초보분석;기중,광학순단삼소적간단、고효、고선택성합성잉연시약물화학화유궤화학관주적중점。신적합성방법화유관단삼소상세적구효관계연구,대개발단삼소류약물구유중요의의。
Danshensu,the active component of Danshen,is a kind of organic compound with simple but particular chemical structure,and widespread physiological and pharmacological activities,es-pecially in the anti-myocardial ischemia and liver protection.However,the sources of Danshensu (or its derivatives)which are isolated from Danshen are limited and could not satisfied the clini-cal need.Therefore,how to synthesis Danshensu(or its derivatives)simply and effectively using chemical methods is the crucial problem needing to be solved during the process of drug develop-ment.In the essay,the relative reports in recent years were reviewed and the synthesis pathway for racemic body and optic pure danshensu were discussed,the structure-function relationship were primarily analyzed,among them,how to synthesis optic pure danshensu using simply,high effective and selective method remain to be the focus of medical chemistry and organic chemis-try.The study regarding novel synthesis methods and detailed exploration of structure-function relationship would provide basis for the development of Danshensu-like drugs.