摘要
生物电子等排是药物结构优化中最常见的一种策略,随着药物化学和有机化学的发展,越来越多的经典的和非经典的生物电子等排体被运用到新药的设计中,近几年来,含氟基团作为生物电子等排体越来越受到药物化学家们的重视,本文扼要地综述二氟甲基(CF_(2)H)的理化性质、化学制备方法及其在药物设计中的应用,旨在为新药研究人员提供参考。
Bioisosterism is one of the most common strategies in drug structure optimization.With the development of medicinal and organic chemistry,more and more classic and non-classical bioisosteres are used in the design of novel drugs.In recent years,fluorinated groups as a bioisostere have been paid more and more attention by pharmaceutical chemists.This paper briefly reviews the physicochemical properties,chemical preparation methods of difluoromethyl(CF_(2)H)group,and its application in drug design to provide references for drug discovery researchers.
作者
张寅生
ZHANG Yin-sheng(Institute for Innovative Drug Discovery,Jiangsu Key Laboratory of Targeted Antiviral Research,Chia Tai Tianqing Pharmaceutical Group Co.,LTD.,Nanjing 211122,China)
出处
《药学学报》
CAS
CSCD
北大核心
2021年第8期2182-2196,共15页
Acta Pharmaceutica Sinica
基金
江苏省科技厅/省重点实验室([2019]No.1627).