文献类型：期刊文献

英文题名：The Application of Bicyclo[11.1]pentane as a Bioisostere of the Phenyl Ring in Pharmaceutical Chemistry

作者：Fang, Zhuohan[1]; Xu, Qian[1]; Lu, Xuehe[2]; Wan, Nianfeng[1]; Yang, Wu-Lin[1]

机构：[1] Shanghai Key Laboratory of Chemical Biology, School of Pharmacy, East China University of Science and Technology, 130 Meilong Road, Shanghai, 200237, China; [2] Frontiers Science Center for Transformative Molecules, Zhangjiang Institute for Advanced Study, Shanghai Jiao Tong University, 429 Zhangheng Lu, Shanghai, 200444, China

年份：2024

卷号：57

期号：6

起止页码：1171

外文期刊名：Synthesis (Germany)

收录：EI(收录号：20244017135323)

语种：英文

外文关键词：Bioactivity

摘要：Bicyclo[1.1.1]pentane (BCP) is a bridging ring skeleton with three-dimensional structure. BCP is a bioisostere of the phenyl ring, tert -butyl group, and alkynes; it has excellent physical and chemical properties compared with phenyl ring, so it has been widely considered by the pharmaceutical chemistry. This short review examines related reports of BCP as a bioisostere of the phenyl ring, and the changes in physicochemical properties and biological activity after substitution. The solubility, clogP, and metabolic toxicity of the drug are improved by BCP bioisosteres, but the biological activity of BCP is lower than the phenyl ring. The application of BCP in drug research and development will be further expanded to provide more possibilities for future drug innovation and development. 1 Introduction 2 Replacement of Phenyl Rings by BCP 3 Conclusion. ? 2024. Thieme. All rights reserved.