Bioorganic & medicinal chemistry letters, 2011-09, Vol.21 (18), p.5423-5427
2011
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Details
- Autor(en) / Beteiligte
- Titel
- Synthesis and biological activity of a novel class nicotinic acetylcholine receptors (nAChRs) ligands structurally related to anatoxin-a
- Ist Teil von
- Bioorganic & medicinal chemistry letters, 2011-09, Vol.21 (18), p.5423-5427
- Ort / Verlag
- Amsterdam: Elsevier Ltd
- Erscheinungsjahr
- 2011
- Quelle
- MEDLINE
- Beschreibungen/Notizen
- The introduction of the isoxazole ring as bioisosteric replacement of the acetyl group of anatoxin-a led to a new series of derivatives binding to nicotinic acetylcholine receptors. Bulkier substitutions than methyl at the 3 position of isoxazole were shown to be detrimental for the activity. The binding potency of the most interesting compounds with α1, α7 and α3β4 receptor subtypes, was, anyway, only at micromolar level. Moreover, differently from known derivatives with pyridine, isoxazole condensed to azabicyclo ring led to no activity.
- Sprache
- Englisch
- Identifikatoren
- ISSN: 0960-894XeISSN: 1464-3405DOI: 10.1016/j.bmcl.2011.06.127Titel-ID: cdi_proquest_miscellaneous_907181491
- Format
- –
- Schlagworte
- Anatoxin-a derivatives, bioactive properties, Biological and medical sciences, chemistry, Chemistry Techniques, Synthetic, cholinergic receptors, Cholinergic system, Dose-Response Relationship, Drug, Ligands, Medical sciences, Molecular Conformation, Neuropharmacology, Neurotransmitters. Neurotransmission. Receptors, Nicotinic acetylcholine receptors ligands, Pharmacology. Drug treatments, pyridines, Receptors, Nicotinic - metabolism, Stereoisomerism, Structure-Activity Relationship, Therapeutic agents for CNS degenerative disorders, Tropanes - chemistry