Synthesis and SAR of novel, non-MPEP chemotype mGluR5 NAMs identified by functional HTS.

Zhou Y, Rodriguez AL, Williams R, Weaver CD, Conn PJ, Lindsley CW
Bioorg Med Chem Lett. 2009 19 (23): 6502-6

PMID: 19875287 · PMCID: PMC3177597 · DOI:10.1016/j.bmcl.2009.10.059

This Letter describes the discovery and SAR of three novel series of mGluR5 non-competitive antagonists/negative allosteric modulators (NAMs) not based on manipulation of an MPEP/MTEP chemotype identified by a functional HTS approach. This work demonstrates fundamentally new mGluR5 NAM chemotypes with submicromolar potencies, and further examples of a mode of pharmacology 'switch' to provide PAMs with a non-MPEP scaffold.

MeSH Terms (10)

Benzamides Benzimidazoles High-Throughput Screening Assays Molecular Structure Phthalimides Pyridines Receptor, Metabotropic Glutamate 5 Receptors, Metabotropic Glutamate Structure-Activity Relationship Thiazoles

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