Synthesis and SAR of a novel positive allosteric modulator (PAM) of the metabotropic glutamate receptor 4 (mGluR4).

Williams R, Johnson KA, Gentry PR, Niswender CM, Weaver CD, Conn PJ, Lindsley CW, Hopkins CR
Bioorg Med Chem Lett. 2009 19 (17): 4967-70

PMID: 19640716 · PMCID: PMC2752865 · DOI:10.1016/j.bmcl.2009.07.072

This Letter describes the synthesis and SAR of the novel positive allosteric modulator, VU0155041, a compound that has shown in vivo efficacy in rodent models of Parkinson's disease. The synthesis takes advantage of an iterative parallel synthesis approach to rapidly synthesize and evaluate a number of analogs of VU0155041.

MeSH Terms (10)

Allosteric Regulation Allosteric Site Anilides Animals Cyclohexanecarboxylic Acids Disease Models, Animal Parkinson Disease Rats Receptors, Metabotropic Glutamate Structure-Activity Relationship

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