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. 2010 Dec 15;20(24):7381-4.
doi: 10.1016/j.bmcl.2010.10.036. Epub 2010 Oct 21.

4-aryl piperazine and piperidine amides as novel mGluR5 positive allosteric modulators

Hui Xiong  1 , Todd A Brugel, Michael Balestra, Dean G Brown, Kelly A Brush, Caprice Hightower, Lindsay Hinkley, Valerie Hoesch, James Kang, Gerard M Koether, John P McCauley Jr, Francis M McLaren, Laura M Panko, Thomas R Simpson, Reed W Smith, James M Woods, Becky Brockel, Vijay Chhajlani, Reto A Gadient, Nathan Spear, Linda A Sygowski, Minli Zhang, Jalaj Arora, Nathalie Breysse, Julie M Wilson, Methvin Isaac, Abdelmalik Slassi, Megan M King
Affiliations

4-aryl piperazine and piperidine amides as novel mGluR5 positive allosteric modulators

Hui Xiong et al. Bioorg Med Chem Lett. .

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.

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