PYRIDYL ETHERS AND THIOETHERS AS LIGANDS FOR NICOTINIC ACETYLCHOLINE RECEPTOR AND ITS THERAPEUTIC APPLICATION
The present invention provides compounds of the formula:wherein m is 0, 1 or 2; p is 0 or 1; Y is O, S, S(O) or S(O)2 and R1 to R7 are various substituents as selective modulators of the nicotinic acetylcholine receptor useful in the treatment of pain, Al
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Page 14
(2010/02/07)
Pyridyl ethers and thioethers as ligands for nicotinic acetylcholine receptor and its therapeutic application
The present invention provides compounds of the formula: wherein m is 0, 1 or 2; p is 0 or 1; Y is O, S, S(O) or S(O)2 and R1 to R7 are various substituents as selective modulators of the nicotinic acetylcholine receptor u
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(2008/06/13)
Synthesis and structure-activity relationship of novel pyridyl ethers for the nicotinic acetylcholine receptor
The preparation of novel pyridyl ethers as ligands for the nicotinic acetylcholine receptor (nAChR) is described. Variations of the ring size of the azacycle and substitution on the pyridine had dramatic effects on receptor binding affinity with IC50S at the α4β2 nAChR ranging from 22 to >10,000 nM. The most potent molecule was (R)-2-chloro-3-(4-cyanophenyl)-5-((3-pyrrolidinyl)oxy)pyridine 27f with an IC50 of 22 nM. (C) 2000 Elsevier Science Ltd. All rights reserved.
Lee, Jung,Davis, Coralie B.,Rivero, Ralph A.,Reitz, Allen B.,Shank, Richard P.
p. 1063 - 1066
(2007/10/03)
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