Department of Molecular Therapeutics and Translational Research Institute, The Scripps Research Institute, Scripps Florida, Jupiter, FL 33458, USA.
Bioorg Med Chem Lett. 2012 Jun 1;22(11):3739-42. doi: 10.1016/j.bmcl.2012.04.023. Epub 2012 Apr 13.
The design and synthesis of a novel series of Rev-erbα agonists is described. The development and optimization of the tetrahydroisoquinoline series was carried out from an earlier acyclic series of Rev-erbα agonists. Through the optimization of the scaffold 1, several potent compounds with good in vivo profiles were discovered.
本文描述了一种新型 Rev-erbα 激动剂的设计和合成。从早期的非环系列 Rev-erbα 激动剂出发，对四氢异喹啉系列进行了开发和优化。通过对骨架 1 的优化，发现了几种具有良好体内特性的有效化合物。
