Syntheses of 2-amino and 2-halothiazole derivatives as high-affinity metabotropic glutamate receptor subtype 5 ligands and potential radioligands for in vivo imaging
FG Siméon, MT Wendahl, VW Pike
Index: Simeon, Fabrice G.; Wendahl, Matthew T.; Pike, Victor W. Journal of Medicinal Chemistry, 2011 , vol. 54, # 3 p. 901 - 908
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Citation Number: 9
Abstract
The structure of the potent selective mGlu5 ligand, SP203 (1, 3-fluoro-5-[[2-(fluoromethyl) thiazol-4-yl] ethynyl] benzonitrile), was modified by replacing the 2-fluoromethyl substituent with an amino or halo substituent and by variation of substituents in the distal aromatic ring to provide a series of new high-affinity mGlu5 ligands. In this series, among the most potent ligands obtained, the 2-chloro-thiazoles 7a and 7b and the 2-fluorothiazole 10b showed ...
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