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

…, M Balestra, DG Brown, KA Brush, C Hightower…

Index: 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 Jr., 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. Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 24 p. 7381 - 7384

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Citation Number: 25

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 ...