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

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.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Xiong H,Brugel TA,Balestra M,Brown DG,Brush KA,Hightower C,Hinkley L,Hoesch V,Kang J,Koether GM,McCauley JP Jr,McLaren FM,Panko LM,Simpson TR,Smith RW,Woods JM,Brockel B,Chhajlani V,Gadient RA,Spear N,Sygowski LA

doi

10.1016/j.bmcl.2010.10.036

subject

Has Abstract

pub_date

2010-12-15 00:00:00

pages

7381-4

issue

24

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(10)01487-3

journal_volume

20

pub_type

杂志文章

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