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

Bioorganic and Medicinal Chemistry Letters

Volumn 19, Issue 8, 2009, Pages 2235-2239

  Thomson, Joanne L ^a   Blackaby, Wesley P ^a   Jennings, Andrew S R ^a   Goodacre, Simon C ^a   Pike, Andrew ^a   Thomas, Steve ^a   Brown, Terry A ^a   Smith, Alison ^a   Pillai, Gopalan ^a   Street, Leslie J ^a   Lewis, Richard T ^a  

^a NEUROSCIENCE RESEARCH CENTRE   (United Kingdom)

Author keywords

Bioavailable; Glycine transporter; GLYT1; Inhibitor; NMDA; Pharmacokinetics; Schizophrenia

Indexed keywords

CYCLOHEXANE DERIVATIVE; GLYCINE TRANSPORTER 1; GLYCINE TRANSPORTER TYPE 1 INHIBITOR; PROTEIN INHIBITOR; SULFONE DERIVATIVE; UNCLASSIFIED DRUG;

ARTICLE; DRUG CLEARANCE; DRUG DISTRIBUTION; DRUG HALF LIFE; DRUG POTENCY; DRUG RECEPTOR BINDING; DRUG SELECTIVITY; DRUG STRUCTURE; DRUG SYNTHESIS; IC 50; NONHUMAN; PROCESS OPTIMIZATION; STRUCTURE ACTIVITY RELATION; STRUCTURE ANALYSIS;

ADMINISTRATION, ORAL; ANIMALS; BIOLOGICAL AVAILABILITY; GLYCINE PLASMA MEMBRANE TRANSPORT PROTEINS; HUMANS; MALE; MICROSOMES, LIVER; RATS; RATS, SPRAGUE-DAWLEY; SULFONAMIDES; TRIAZOLES;

EID: 63149136505     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2009.02.102     Document Type: Article

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