有机化学 ›› 2007, Vol. 27 ›› Issue (11): 1366-1368. 上一篇    下一篇

研究论文

Hirsutellide A立体异构体的单晶结构与抗分支杆菌生物活性研究

许艳杰a,李江胜b,颜范勇b,陈立功*,a   

  1. (a天津大学化工学院 天津 300072)
    (b天津大学药物科学与技术学院 天津 300072)
  • 收稿日期:2007-01-24 修回日期:2007-03-23 发布日期:2007-10-20
  • 通讯作者: 陈立功

Study on X-ray Crystallography and Antimycobacterial Bioactivity of the Stereoisomer of Hirsutellide A

XU Yan-Jiea,LI Jiang-Shengb,YAN Fan-Yongb,CHEN Li-Gong*,a   

  1. (a School of Chemical Engineering and Technology, Tianjin University, Tianjin 300072)
    (b School of Pharmaceutical Science and Technology, Tianjin University, Tianjin 300072)
  • Received:2007-01-24 Revised:2007-03-23 Published:2007-10-20
  • Contact: CHEN Li-Gong

研究了hirsutellide A立体异构体的X衍射单晶结构及其抗分支杆菌活性. 该化合物具有扭曲马鞍型18元大环结构; 在体外生物活性测试中, 化合物未表现出明显的抗分支杆菌活性. 由实验结果可以看出在天然环酯肽hirsutellide A中3'-C手性中心是其生物活性关键位点之一.

关键词: hirsutellide A, 单晶结构, 生物活性, 环六酯肽, 抗分支杆菌

X-ray crystallography and antimycobacterial activity of a cyclohexadepsipeptide, one of the stereoisomers of hirsutellide A, were studied. Its single crystal structure reveals that the 18 membered macrocycle has a distorted saddle shape. The cyclopeptide exhibited no significant antimycobacterial activity in vitro. It was concluded that the chiral center of 3'-C was one of the pivotal factor in hirsutellide A for its biological activity.

Key words: single crystal structure, biological activity, cyclohexadepsipeptide, antimycobacterial, hirsutellide A