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Bioorg Med Chem Lett ; 21(16): 4891-9, 2011 Aug 15.
Article in English | MEDLINE | ID: mdl-21757343

ABSTRACT

A series of 6-aryl-3-pyrrolidinylpyridine analogs was explored as structurally novel negative allosteric modulators of the mGlu5 receptor lacking an alkyne or oxadiazole moiety. Compounds in this series were characterized by tractable SAR, good in vitro potencies and brain penetration in rodents.


Subject(s)
Pyridines/pharmacology , Pyrrolidines/pharmacology , Receptors, Metabotropic Glutamate/antagonists & inhibitors , Animals , Dose-Response Relationship, Drug , HEK293 Cells , Humans , Models, Molecular , Molecular Structure , Pyridines/chemical synthesis , Pyridines/chemistry , Pyrrolidines/chemical synthesis , Pyrrolidines/chemistry , Rats , Rats, Sprague-Dawley , Receptor, Metabotropic Glutamate 5 , Receptors, Metabotropic Glutamate/blood , Stereoisomerism , Structure-Activity Relationship
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