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

Rocco D. Gogliotti; Anna L. Blobaum; Ryan M. Morrison; J. Scott Daniels; James M. Salovich; Yiu Yin Cheung; Alice L. Rodriguez; Matthew T. Loch; P. Jeffrey Conn; Craig W. Lindsley; Colleen M. Niswender; Corey R. Hopkins

doi:10.1016/j.bmcl.2016.05.029

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

Rocco D. Gogliotti, Anna L. Blobaum, Ryan M. Morrison, J. Scott Daniels, James M. Salovich, Yiu Yin Cheung, Alice L. Rodriguez, Matthew T. Loch, P. Jeffrey Conn, Craig W. Lindsley, Colleen M. Niswender, Corey R. Hopkins

Research output: Contribution to journal › Article › peer-review

5 Scopus citations

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)
Pages (from-to)	2984-2987
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	26
Issue number	13
DOIs	https://doi.org/10.1016/j.bmcl.2016.05.029
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

Access to Document

10.1016/j.bmcl.2016.05.029

Cite this

Gogliotti, R. D., Blobaum, A. L., Morrison, R. M., Daniels, J. S., Salovich, J. M., Cheung, Y. Y., Rodriguez, A. L., Loch, M. T., Conn, P. J., Lindsley, C. W., Niswender, C. M., & Hopkins, C. R. (2016). Discovery and characterization of a novel series of N-phenylsulfonyl-1H-pyrrole picolinamides as positive allosteric modulators of the metabotropic glutamate receptor 4 (mGlu₄). Bioorganic and Medicinal Chemistry Letters, 26(13), 2984-2987. https://doi.org/10.1016/j.bmcl.2016.05.029

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, Rocco D.; Blobaum, Anna L.; Morrison, Ryan M. et al.
In: Bioorganic and Medicinal Chemistry Letters, Vol. 26, No. 13, 01.07.2016, p. 2984-2987.

Research output: Contribution to journal › Article › peer-review

Gogliotti, RD, Blobaum, AL, Morrison, RM, Daniels, JS, Salovich, JM, Cheung, YY, Rodriguez, AL, Loch, MT, Conn, PJ, Lindsley, CW, Niswender, CM & Hopkins, CR 2016, 'Discovery and characterization of a novel series of N-phenylsulfonyl-1H-pyrrole picolinamides as positive allosteric modulators of the metabotropic glutamate receptor 4 (mGlu₄)', Bioorganic and Medicinal Chemistry Letters, vol. 26, no. 13, pp. 2984-2987. https://doi.org/10.1016/j.bmcl.2016.05.029

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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.",

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AU - Morrison, Ryan M.

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AU - Salovich, James M.

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