1,3-Diaminopropan-2-ol Sulfonamides as potent and selective inhibitors of the glycine transporter type 1

High throughput screening led to the discovery of a novel series of 1,3-diaminopropan-2-ol sulfonamides as selective GlyT-1 inhibitors. Structure–activity relationships of this novel series and optimisation of the initial hit that led to the identification of ( 2), a potent and selective GlyT-1 inhi...

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Bibliographic Details
Published inBioorganic & medicinal chemistry letters Vol. 17; no. 6; pp. 1741 - 1745
Main Authors Rahman, Shahzad S., Coulton, Steven, Herdon, Hugh J., Joiner, Graham F., Jin, Jian, Porter, Roderick A.
Format Journal Article
LanguageEnglish
Published Oxford Elsevier Ltd 15.03.2007
Elsevier
Subjects
1,3-Diaminopropan-2-ol
Animals
Biological and medical sciences
Cell Line, Tumor
Chromatography, High Pressure Liquid
Computer Simulation
Drug Evaluation, Preclinical
Glycine Plasma Membrane Transport Proteins - antagonists & inhibitors
GlyT-1
Humans
Isomerism
Medical sciences
Miscellaneous
Molecular Conformation
NMDA
Pharmacology. Drug treatments
Rats
Schizophrenia
Spectrophotometry, Ultraviolet
Structure-Activity Relationship
Sulfonamides - chemical synthesis
Sulfonamides - pharmacology
Transporter
1,3-Diaminopropan-2-ol
Schizophrenia
NMDA
GlyT-1
High throughput screening
Aminoalcohol
Sulfonamide
GLYT1 glycine transporter
Biological transport
GlyT-1; Schizophrenia; NMDA
Glutamate receptor
Selectivity
In vitro
Naphthalene derivatives
Optimization
Psychosis
Structure activity relation
Piperidine derivatives
Inhibitor
Secondary alcohol
NMDA receptor
Transporter; 1,3-Diaminopropan-2-ol
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Summary:High throughput screening led to the discovery of a novel series of 1,3-diaminopropan-2-ol sulfonamides as selective GlyT-1 inhibitors. Structure–activity relationships of this novel series and optimisation of the initial hit that led to the identification of ( 2), a potent and selective GlyT-1 inhibitor, are also presented. High throughput screening led to the discovery of a novel series of 1,3-diaminopropan-2-ol sulfonamides as selective GlyT-1 inhibitors. Structure–activity relationships of this novel series and optimisation of the initial hit that led to the identification of ( 2), a potent and selective GlyT-1 inhibitor, are also presented.
Bibliography:ObjectType-Article-1
SourceType-Scholarly Journals-1
ObjectType-Feature-2
content type line 23
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2006.12.063