Biososteric Replacement in the Design and Synthesis of Ligands for Nicotinic Acetylcholine Receptors
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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 dialkylamino and appropriately substituted benzene rings (NO2, 8; OH, 9) are bioisosteric replacements for pyrrolidine and pyridine, respectively.
KeywordsEther Benzene Nicotine Pyridine Acetylcholine
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