Literature DB >> 19318248

Optimisation of a series of potent, selective and orally bioavailable GlyT1 inhibitors.

Joanne L Thomson1, 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.   

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.

Entities:  

Mesh:

Substances:

Year:  2009        PMID: 19318248     DOI: 10.1016/j.bmcl.2009.02.102

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  1 in total

1.  Identification of an Orally Bioavailable, Potent, and Selective Inhibitor of GlyT1.

Authors:  Wesley P Blackaby; Richard T Lewis; Joanne L Thomson; Andrew S R Jennings; Simon C Goodacre; Leslie J Street; Angus M MacLeod; Andrew Pike; Suzanne Wood; Steve Thomas; Terry A Brown; Alison Smith; Gopalan Pillai; Sarah Almond; Martin R Guscott; H Donald Burns; Waisi Eng; Christine Ryan; Jacquelynn Cook; Terence G Hamill
Journal:  ACS Med Chem Lett       Date:  2010-06-25       Impact factor: 4.345

  1 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.