Abstract：
The use of privileged scaffolds in medicinal chemistry is an effective way to accelerate the drug discovery process, especially at the hit/lead optimization stage. 2-Phenylcyclopropylmethylamine (PCPMA) is a less commonly used chemical scaffold in medicinal chemistry, but many PCPMA-containing compounds exert therapeutic effects for various diseases, in particular central nervous system (CNS) diseases such as depression, schizophrenia, sleep disorder, and Parkinson\'s disease. The backbone of the PCPMA scaffold enables a unique structure of an amino group linked to a benzene ring through an alkyl linker, making it a useful template for the design of bioactive compounds especially for CNS drug targets including aminergic GPCRs and transporters. This review summarizes the medicinal chemistry studies of PCPMA-containing drugs and drug-like molecules, their mechanisms of action, and biological activities. We conclude that PCPMA is a unique and useful privileged scaffold for CNS drug design.
摘要：
在药物化学中使用特权支架是加速药物发现过程的有效途径，特别是在命中/领先优化阶段。2-苯基环丙基甲胺（PCPMA）是药物化学中不常用的化学支架，但是许多含有PCPMA的化合物对各种疾病都有治疗作用，特别是中枢神经系统（CNS）疾病，如抑郁症，精神分裂症,睡眠障碍,和帕金森病。PCPMA支架的骨架能够实现通过烷基接头与苯环连接的氨基的独特结构，使其成为设计生物活性化合物的有用模板，特别是用于CNS药物靶标，包括胺能GPCRs和转运蛋白。本文综述了含PCPMA的药物和药物样分子的药物化学研究，他们的行动机制，和生物活动。我们得出结论，PCPMA是CNS药物设计的独特且有用的特权支架。
