首页 | 本学科首页   官方微博 | 高级检索  
     


Optimisation of a series of potent,selective and orally bioavailable GlyT1 inhibitors
Authors:Joanne L. Thomson  Wesley P. Blackaby  Andrew S.R. Jennings  Simon C. Goodacre  Andrew Pike  Steve Thomas  Terry A. Brown  Alison Smith  Gopalan Pillai  Leslie J. Street  Richard T. Lewis
Affiliation:Department of Medicinal Chemistry, Merck Sharp and Dohme, Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, UK
Abstract:A series of heterocyclic sulfonamides have been developed which are potent and selective inhibitors of hGlyT1. SAR studies to optimise the in vitro and in vivo properties are described. Optimisation of the central scaffold resulted in cyclohexane sulfones 28 and 29, which have good PK properties and show promise for further development.
Keywords:
本文献已被 ScienceDirect 等数据库收录!
设为首页 | 免责声明 | 关于勤云 | 加入收藏

Copyright©北京勤云科技发展有限公司  京ICP备09084417号