Discovery and characterization of a novel series of N-phenylsulfonyl-1H-pyrrole picolinamides as positive allosteric modulators of the metabotropic glutamate receptor 4 (mGlu4).

Gogliotti RD, Blobaum AL, Morrison RM, Daniels JS, Salovich JM, Cheung YY, Rodriguez AL, Loch MT, Conn PJ, Lindsley CW, Niswender CM, Hopkins CR
Bioorg Med Chem Lett. 2016 26 (13): 2984-2987

PMID: 27234146 · PMCID: PMC4955388 · DOI:10.1016/j.bmcl.2016.05.029

Herein we report the synthesis and characterization of a novel series of N-phenylsulfonyl-1H-pyrrole picolinamides as novel positive allosteric modulators of mGlu4. We detail our work towards finding phenyl replacements for the core scaffold of previously reported phenyl sulfonamides and phenyl sulfone compounds. Our efforts culminated in the identification of N-(1-((3,4-dimethylphenyl)sulfonyl)-1H-pyrrol-3-yl)picolinamide as a potent PAM of mGlu4.

Copyright © 2016 Elsevier Ltd. All rights reserved.

MeSH Terms (10)

Allosteric Regulation Animals Microsomes, Liver Picolinic Acids Pyrroles Rats Receptors, Metabotropic Glutamate Structure-Activity Relationship Sulfonamides Triazoles

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