2,5-Disubstituted pyridines: the discovery of a novel series of 5-HT2A ligands |
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| Authors: | Wilson Kevin J van Niel Monique B Cooper Laura Bloomfield Dawn O'Connor Desmond Fish L Rebecca MacLeod Angus M |
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| Institution: | The Neuroscience Research Centre, Merck Sharp and Dohme, Terlings Park, Harlow, Essex CM20 2QR, UK. kevin_wilson2@merck.com |
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| Abstract: | This report describes the effect of replacing the central basic amine present in many known 5-HT(2A) ligands with an aromatic residue. We targeted the isomeric phenethylpyridines 2 and 3 and these compounds proved to be excellent leads, possessing good 5-HT(2A) receptor binding affinity and selectivity over the 5-HT(2C) subtype. Optimization of one isomer led to the identification of 25, a compound with sub-nanomolar 5-HT(2A) affinity and selectivity over 5-HT(2C) of greater than 4600-fold. |
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