Bioorganic & medicinal chemistry letters, 2004-03, Vol.14 (5), p.1213-1216
2004
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Details
- Autor(en) / Beteiligte
- Titel
- Subtype selective NMDA receptor antagonists: evaluation of some novel alkynyl analogues
- Ist Teil von
- Bioorganic & medicinal chemistry letters, 2004-03, Vol.14 (5), p.1213-1216
- Ort / Verlag
- Oxford: Elsevier
- Erscheinungsjahr
- 2004
- Quelle
- MEDLINE
- Beschreibungen/Notizen
- A benzylpiperidine analogue with an acetylenic linker, 5-(3-[4-(4-fluorobenzyl)-piperidin-1-yl]-prop-1-ynyl)-1,3-dihydrobenzimidazol-2-one (3), was identified as a chemical lead with excellent activity at the NR1A/2B receptor (IC50=3 nM). Efforts to optimize this activity led to focused modifications around the structural motif of 3. The synthesis and SAR studies are discussed.
- Sprache
- Englisch
- Identifikatoren
- ISSN: 0960-894XeISSN: 1464-3405DOI: 10.1016/j.bmcl.2003.12.049Titel-ID: cdi_proquest_miscellaneous_80179484
- Format
- –
- Schlagworte
- Alkynes - chemistry, Alkynes - metabolism, Alkynes - pharmacology, Animals, Biological and medical sciences, Brain - drug effects, Brain - metabolism, Drug Evaluation, Preclinical - methods, Excitatory Amino Acid Antagonists - chemistry, Excitatory Amino Acid Antagonists - metabolism, Excitatory Amino Acid Antagonists - pharmacology, Glutamatergic system (aspartate and other excitatory aminoacids), Medical sciences, Neuropharmacology, Neurotransmitters. Neurotransmission. Receptors, Pharmacology. Drug treatments, Rats, Receptors, N-Methyl-D-Aspartate - antagonists & inhibitors, Receptors, N-Methyl-D-Aspartate - metabolism