1.
ACS Med Chem Lett
; 1(7): 350-4, 2010 Oct 14.
Article
in English
| MEDLINE
| ID: mdl-24900218
ABSTRACT
Amalgamation of the structure-activity relationship of two series of GlyT1 inhibitors developed at Merck led to the discovery of a clinical candidate, compound 16 (DCCCyB), which demonstrated excellent in vivo occupancy of GlyT1 transporters in rhesus monkey as determined by displacement of a PET tracer ligand.
2.
Bioorg Med Chem Lett
; 19(8): 2235-9, 2009 Apr 15.
Article
in English
| MEDLINE
| ID: mdl-19318248
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.