Abstract
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.
Original language | English (US) |
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Pages (from-to) | 2984-2987 |
Number of pages | 4 |
Journal | Bioorganic and Medicinal Chemistry Letters |
Volume | 26 |
Issue number | 13 |
DOIs | |
State | Published - Jul 1 2016 |
Externally published | Yes |
Keywords
- Metabotropic glutamate receptor 4
- PK
- Phenyl replacement
- Positive allosteric modulator (PAM)
- Pyrrole sulfonamide
ASJC Scopus subject areas
- Biochemistry
- Molecular Medicine
- Molecular Biology
- Pharmaceutical Science
- Drug Discovery
- Clinical Biochemistry
- Organic Chemistry