Positive allosteric modulators(PAMs) of metabotropic glutamate 2 receptor (mGluR2), which bind at an alternative site to the orthosteric endogenous agonist, may have advantages such as increasing mGluR2 signaling with greater selectivity, maintaining activity based on transient and dynamic release of glutamate without inducing over-activation or desensitization. Herein we report a series of novel substituted phenylcyclopropylmethyl triazolopyridinamines. The syntheses and the SAR of these compounds will be discussed. Some of the compounds reversed PCP stimulated locomotor activity and were also active in Y-maze test. Those compounds that showed <i>in vivo</i> activity had also good metabolic stabilities and brain exposures.

Synthesis and SAR studies of positive allosteric modulators of mGluR2 for treatment of neurological and psychiatric diseases

254th National Meeting (2017)

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