Bioorganic & medicinal chemistry letters, 2002-07, Vol.12 (13), p.1755
2002
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Details
- Autor(en) / Beteiligte
- Titel
- 4,4-Disubstituted cyclohexylamine NK(1) receptor antagonists I
- Ist Teil von
- Bioorganic & medicinal chemistry letters, 2002-07, Vol.12 (13), p.1755
- Ort / Verlag
- England
- Erscheinungsjahr
- 2002
- Quelle
- Access via ScienceDirect (Elsevier)
- Beschreibungen/Notizen
- A series of novel 4,4-disubstituted cyclohexylamine based NK(1) antagonists is described. The effect of changes to the C(1)-C(4) relative stereochemistry on the cyclohexane ring and replacements for the flexible linker are discussed, leading to the identification of compounds with high affinity and good in vivo duration of action.
- Sprache
- Englisch
- Identifikatoren
- ISSN: 0960-894XTitel-ID: cdi_pubmed_primary_12067554
- Format
- –
- Schlagworte
- Animals, Binding Sites, Central Nervous System - drug effects, Central Nervous System - metabolism, CHO Cells, Cricetinae, Cyclohexylamines - chemical synthesis, Cyclohexylamines - pharmacokinetics, Cyclohexylamines - pharmacology, Gerbillinae, Inhibitory Concentration 50, Molecular Conformation, Neurokinin-1 Receptor Antagonists, Radioligand Assay, Receptors, Neurokinin-1 - chemistry, Structure-Activity Relationship