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影响喹诺酮C—4位构效关系的若干因素
引用本文:李江波,林瑞森.影响喹诺酮C—4位构效关系的若干因素[J].化学研究与应用,1999,11(3):279-281.
作者姓名:李江波  林瑞森
作者单位:浙江大学化学系
摘    要:喹诺酮类药物是两类重要抗生素之一,此类化合物的结构见图1。虽然喹诺酮不同位置的结构修饰已涌现出许多广谱、高效、低毒性的化疗药物,如诺氟沙星、环丙沙星、氧氟沙星等[1]。但对C-4位的修饰却未能成功:C-4位酮基被硫酮基、亚胺基取代均使活性消失[2];...

关 键 词:喹诺酮  构效关系  分子力学  AM1

SOME FACTORS INFLUENCING ON THE STRUCTUREACTIVITY RELATIONSHIP OF C4 POSITIN OF QUINOLONE
Li JiangboLin RuisenYu Qingsen.SOME FACTORS INFLUENCING ON THE STRUCTUREACTIVITY RELATIONSHIP OF C4 POSITIN OF QUINOLONE[J].Chemical Research and Application,1999,11(3):279-281.
Authors:Li JiangboLin RuisenYu Qingsen
Abstract:In this paper,the structure-activity relationship of c-4 position of quinolone and its analogues was sdudied by MM and AM1.The results showed that the coplanarity of the parent nucleus,the coplanarity between the group of c-4 position and the parent mucleus,the coplanarity between carboxy1 and keto group are all very important to biologcal activities.
Keywords:guinolone  structure-activity relationship  MM  AM1
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