文献类型：期刊文献

英文题名：The Application of Bicyclo[1.1.1]pentane as a Bioisostere of the Phenyl Ring in Pharmaceutical Chemistry

作者：Fang, Zhuohan[1,2];Xu, Qian[1,2];Lu, Xuehe[3];Wan, Nianfeng[1,2];Yang, Wu-Lin[1,2]

机构：[1]East China Univ Sci & Technol, Shanghai Key Lab Chem Biol, 130 Meilong Rd, Shanghai 200237, Peoples R China;[2]East China Univ Sci & Technol, Sch Pharm, 130 Meilong Rd, Shanghai 200237, Peoples R China;[3]Shanghai Jiao Tong Univ, Zhangjiang Inst Adv Study, Frontiers Sci Ctr Transformat Mol, 429 Zhangheng Lu, Shanghai 200444, Peoples R China

年份：2025

卷号：57

期号：06

起止页码：1171

外文期刊名：SYNTHESIS-STUTTGART

收录：;WOS:【SCI-EXPANDED(收录号:WOS:001317193000003)】；

基金：This work is supported by Shanghai Agriculture Applied Technology Development Program (T2023309) and the National Natural Science Foundation of China (22171081).

语种：英文

外文关键词：bicyclo[1.1.1]pentane; phenyl ring; bioisosteres; physicochemical properties; pharmaceutical chemistry

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