摘要
多样性合成旨在高效地构建取代基、官能团、立体化学和骨架多样的化合物库,进而发现多样性的生物学效应。本文结合代表性实例,总结了多样性合成的常见策略,包括基于试剂的策略、基于底物的策略、"构建-耦合-配对"策略以及基于优势结构的多样性合成策略。同时,介绍了通过多样性合成构建的化合物库在药物发现中的应用。
Diversity-oriented synthesis(DOS) aims to efficiently generate collections of small molecules with diverse appendages, functional groups, stereochemistry and skeletons, thus yielding diverse biological activities capable of modulating a wide variety of biological processes. In this review, we discussed the common strategies employed in DOS with specific examples from recent literature, including reagent-based approach, substrate-based approach, build-couple-pair strategy and privileged substructure-based DOS. The application of some DOS libraries in drug discovery is also presented.
出处
《药学学报》
CAS
CSCD
北大核心
2015年第4期419-433,共15页
Acta Pharmaceutica Sinica
基金
国家杰出青年科学基金项目(81025017)
关键词
多样性合成
多样性
化学空间
化合物库
药物发现
diversity-oriented synthesis
diversity
chemical space
compound library
drug discovery