| Title : Synthesis and structure-activity relationships of pyridine-modified analogs of 3-[2-((S)-pyrrolidinyl)methoxy]pyridine, A-84543, a potent nicotinic acetylcholine receptor agonist - Lin_1998_Bioorg.Med.Chem.Lett_8_249 |
| Author(s) : Lin NH , Gunn DE , Li Y , He Y , Bai H , Ryther KB , Kuntzweiler T , Donnelly-Roberts D , Anderson DJ , Campbell JE , Sullivan JP , Arneric SP , Holladay MW |
| Ref : Bioorganic & Medicinal Chemistry Lett , 8 :249 , 1998 |
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Abstract :
Analogs of 3-[2-((S)-pyrrolidinyl)methoxy]pyridine, (A-84543, 1) with 2-, 4-, 5-, and 6-substituents on the pyridine ring were synthesized. These analogs exhibited Ki values ranging from 0.15 to > 9,000 nM when tested in vitro for neuronal nicotinic acetylcholine receptor binding activity. Assessment of functional activity at subtypes of neuronal nicotinic acetylcholine receptors indicates that pyridine substitution can have a profound effect on efficacy at these subtypes, and several subtype-selective agonists and antagonists have been identified. |
| PubMedSearch : Lin_1998_Bioorg.Med.Chem.Lett_8_249 |
| PubMedID: 9871663 |
Lin NH, Gunn DE, Li Y, He Y, Bai H, Ryther KB, Kuntzweiler T, Donnelly-Roberts D, Anderson DJ, Campbell JE, Sullivan JP, Arneric SP, Holladay MW (1998)
Synthesis and structure-activity relationships of pyridine-modified analogs of 3-[2-((S)-pyrrolidinyl)methoxy]pyridine, A-84543, a potent nicotinic acetylcholine receptor agonist
Bioorganic & Medicinal Chemistry Lett
8 :249
Lin NH, Gunn DE, Li Y, He Y, Bai H, Ryther KB, Kuntzweiler T, Donnelly-Roberts D, Anderson DJ, Campbell JE, Sullivan JP, Arneric SP, Holladay MW (1998)
Bioorganic & Medicinal Chemistry Lett
8 :249