Biososteric Replacement in the Design and Synthesis of Ligands for Nicotinic Acetylcholine Receptors


A series of ethers containing pyrrolidine and/or pyridine bioisosteres was synthesized and evaluated as nicotinic ligands. The dimethylaminoethoxypridines 6 and 7 inhibited the specific bind of (-)-[3H]Nicotine with Ki values of 300 nM and 450 nM, respectively. Compounds 8 and 9 were found to have Ki values of 3390 nM and 360 nM. These results suggest that… (More)
DOI: 10.1007/s00044-005-0137-8


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