Rational Design, Synthesis and SAR Study of Some Cyclopropane Derivatives as KARI Inhibitors

摘要：

Ketol-acid reductoisomerase (KARI; EC 1. 1. 1. 86) catalyzes the second common step in branched-chain amino acid biosynthesis. The catalyzed process consists of two steps, the first of which is an alkyl migration from one carbon atom to its neighbourring atom. The likely transition state is a cyclopropane derivative, thus a series of new cyclopropane derivatives were designed and synthesized. High throughput virtual screening method was used to find some novel structural KARI inhibitors including cyclopropane structure. The structure-activity relationship was discussed in this paper.

关键词： KARI rational drsign cyclopropane derivatives SAR

作者: Liu Xinghai Chen Peiquan Guo Wancheng Li Yonghong Wang Suhua Li Zhengming

作者单位: The Research Institute of Elemento-organic Chemistry, The State-Key Laboratory of Elemento-organic Chemistry, National Pesticide Engineering Research Center, Nankai University, Tianjin 300071, P. R. China

会议类型: 国际会议

会议名称: 第三届“农药与环境安全国际学术研讨会暨第七届“植物化学保护和全球法律一体化国际研讨会(3rd International Symposium on Pesticide and Environmental Safety & 7th International Workshop on Crop Protection Chemistry and Regulatory Harmonization)

会议地点: 北京

会议语种:英文

页码: 363-368

在线出版日期: 2007-10-09（万方平台首次上网日期，不代表论文的发表时间）