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4-aryl piperazine and piperidine amides as novel mGluR5 positive allosteric modulators.
Xiong, Hui; Brugel, Todd A; Balestra, Michael; Brown, Dean G; Brush, Kelly A; Hightower, Caprice; Hinkley, Lindsay; Hoesch, Valerie; Kang, James; Koether, Gerard M; McCauley, John P; McLaren, Francis M; Panko, Laura M; Simpson, Thomas R; Smith, Reed W; Woods, James M; Brockel, Becky; Chhajlani, Vijay; Gadient, Reto A; Spear, Nathan; Sygowski, Linda A; Zhang, Minli; Arora, Jalaj; Breysse, Nathalie; Wilson, Julie M; Isaac, Methvin; Slassi, Abdelmalik; King, Megan M.
Bioorg Med Chem Lett ; 20(24): 7381-4, 2010 Dec 15.
Article in English | MEDLINE | ID: mdl-21067920

ABSTRACT

Positive allosteric modulation of metabotropic glutamate receptor 5 (mGluR5) is regarded as a potential novel treatment for schizophrenic patients. Herein we report the synthesis and SAR of 4-aryl piperazine and piperidine amides as potent mGluR5 positive allosteric modulators (PAMs). Several analogs have excellent activity and desired drug-like properties. Compound 2b was further characterized as a PAM using several in vitro experiments, and produced robust activity in several preclinical animal models.


Subject(s)
Amides/chemistry , Piperazines/chemistry , Piperidines/chemistry , Receptors, Metabotropic Glutamate/chemistry , Allosteric Regulation , Amides/chemical synthesis , Amides/therapeutic use , Humans , Microsomes, Liver/metabolism , Piperazine , Receptor, Metabotropic Glutamate 5 , Receptors, Metabotropic Glutamate/metabolism , Schizophrenia/drug therapy , Structure-Activity Relationship
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