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Synthesis and structure–activity relationships of 5-substituted pyridine analogues of 3-[2-((S)-pyrrolidinyl)methoxy]pyridine, A-84543
- Source :
- Bioorganic & Medicinal Chemistry Letters. 11:631-633
- Publication Year :
- 2001
- Publisher :
- Elsevier BV, 2001.
-
Abstract
- In an effort to probe the steric influence of C5 substitution of the pyridine ring on CNS binding affinity, analogues of 1 substituted with a bulky moiety—such as phenyl, substituted phenyl, or heteroaryl—were synthesized and tested in vitro for neuronal nicotinic acetylcholine receptor binding affinity. The substituted analogues exhibited K i values ranging from 0.055 to 0.69 nM compared to a K i value of 0.15 nM for compound 1 . Assessment of functional activity at subtypes of neuronal nicotinic acetylcholine receptors led to identify several agonists and antagonists.
- Subjects :
- Steric effects
Chemistry
Stereochemistry
Organic Chemistry
Clinical Biochemistry
Pharmaceutical Science
Ligand (biochemistry)
Biochemistry
Chemical synthesis
chemistry.chemical_compound
Nicotinic acetylcholine receptor
Nicotinic agonist
Drug Discovery
Pyridine
Molecular Medicine
Receptor
Molecular Biology
Acetylcholine receptor
Subjects
Details
- ISSN :
- 0960894X
- Volume :
- 11
- Database :
- OpenAIRE
- Journal :
- Bioorganic & Medicinal Chemistry Letters
- Accession number :
- edsair.doi...........49c642253190ee14ad2d1875f66a4395