Bioorganic & medicinal chemistry letters, 2009-03, Vol.19 (5), p.1492-1495
- Wolkenberg, Scott E.
- Zhao, Zhijian
- Wisnoski, David D.
- Leister, William H.
- O’Brien, Julie
- Lemaire, Wei
- Williams, David L.
- Jacobson, Marlene A.
- Sur, Cyrille
- Kinney, Gene G.
- Pettibone, Doug J.
- Tiller, Philip R.
- Smith, Sheri
- Gibson, Christopher
- Ma, Bennett K.
- Polsky-Fisher, Stacey L.
- Lindsley, Craig W.
- Hartman, George D.
2009
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- Autor(en) / Beteiligte
- Wolkenberg, Scott E.
- Zhao, Zhijian
- Wisnoski, David D.
- Leister, William H.
- O’Brien, Julie
- Lemaire, Wei
- Williams, David L.
- Jacobson, Marlene A.
- Sur, Cyrille
- Kinney, Gene G.
- Pettibone, Doug J.
- Tiller, Philip R.
- Smith, Sheri
- Gibson, Christopher
- Ma, Bennett K.
- Polsky-Fisher, Stacey L.
- Lindsley, Craig W.
- Hartman, George D.
- Titel
- Discovery of GlyT1 inhibitors with improved pharmacokinetic properties
- Ist Teil von
- Bioorganic & medicinal chemistry letters, 2009-03, Vol.19 (5), p.1492-1495
- Ort / Verlag
- England: Elsevier Ltd
- Erscheinungsjahr
- 2009
- Quelle
- MEDLINE
- Beschreibungen/Notizen
- Glycine transporter 1 (GlyT1) represents a novel target for the treatment of schizophrenia via the potentiation of glutamatergic NMDA receptors. The discovery of 4,4-disubstituted piperidine inhibitors of GlyT1 which exhibit improved pharmacokinetic properties, including oral bioavailability, is discussed.
- Sprache
- Englisch
- Identifikatoren
- ISSN: 0960-894XeISSN: 1464-3405DOI: 10.1016/j.bmcl.2009.01.015Titel-ID: cdi_proquest_miscellaneous_66947785
- Format
- –
- Schlagworte
- Animals, Cassette dosing, Dogs, Drug Discovery - methods, Glycine - biosynthesis, Glycine Plasma Membrane Transport Proteins - antagonists & inhibitors, Glycine Plasma Membrane Transport Proteins - metabolism, GlyT1, Humans, Mice, Mice, Inbred DBA, N-Methylaspartate - chemistry, N-Methylaspartate - pharmacology, NMDA pharmacokinetics, Piperidines - administration & dosage, Piperidines - chemical synthesis, Piperidines - pharmacokinetics, Rats, Schizophrenia, Substrate Specificity, Sulfonamides - chemical synthesis