Talele Tanaji T
Department of Pharmaceutical Sciences, College of Pharmacy and Health Sciences, St. John's University , 8000 Utopia Parkway, Queens, New York 11439, United States.
J Med Chem. 2016 Oct 13;59(19):8712-8756. doi: 10.1021/acs.jmedchem.6b00472. Epub 2016 Jun 30.
Recently, there has been an increasing use of the cyclopropyl ring in drug development to transition drug candidates from the preclinical to clinical stage. Important features of the cyclopropane ring are, the (1) coplanarity of the three carbon atoms, (2) relatively shorter (1.51 Å) C-C bonds, (3) enhanced π-character of C-C bonds, and (4) C-H bonds are shorter and stronger than those in alkanes. The present review will focus on the contributions that a cyclopropyl ring makes to the properties of drugs containing it. Consequently, the cyclopropyl ring addresses multiple roadblocks that can occur during drug discovery such as (a) enhancing potency, (b) reducing off-target effects,
最近，环丙基在药物研发中的应用越来越多，用于将候选药物从临床前阶段推进到临床阶段。环丙烷环的重要特征包括：（1）三个碳原子共平面；（2）碳-碳键相对较短（1.51 Å）；（3）碳-碳键的π特性增强；（4）碳-氢键比烷烃中的碳-氢键更短、更强。本综述将聚焦于环丙基对含环丙基药物性质的贡献。因此，环丙基克服了药物发现过程中可能出现的多个障碍，例如（a）增强效力，（b）减少脱靶效应，
