Discovery, Structure–Activity Relationship, and Biological Characterization of a Novel Series of 6-((1H-Pyrazolo[4,3-b]pyridin-3-yl)amino)-benzo[d]isothiazole-3-carboxamides as Positive Allosteric Modulators of the Metabotropic Glutamate Receptor 4 (mGlu4)

Sean R. Bollinger; Darren W. Engers; Joseph D. Panarese; Mary West; Julie L. Engers; Matthew T. Loch; Alice L. Rodriguez; Anna L. Blobaum; Carrie K. Jones; Analisa Thompson Gray; P. Jeffrey Conn; Craig W. Lindsley; Colleen M. Niswender; Corey R. Hopkins

doi:10.1021/acs.jmedchem.8b00994

Discovery, Structure–Activity Relationship, and Biological Characterization of a Novel Series of 6-((1H-Pyrazolo[4,3-b]pyridin-3-yl)amino)-benzo[d]isothiazole-3-carboxamides as Positive Allosteric Modulators of the Metabotropic Glutamate Receptor 4 (mGlu4)

Journal of Medicinal Chemistry ◽

10.1021/acs.jmedchem.8b00994 ◽

2018 ◽

Vol 62 (1) ◽

pp. 342-358 ◽

Cited By ~ 7

Author(s):

Sean R. Bollinger ◽

Darren W. Engers ◽

Joseph D. Panarese ◽

Mary West ◽

Julie L. Engers ◽

...

Keyword(s):

Glutamate Receptor ◽

Metabotropic Glutamate Receptor ◽

Structure Activity Relationship ◽

Activity Relationship ◽

Allosteric Modulators ◽

Biological Characterization ◽

Metabotropic Glutamate ◽

Structure Activity ◽

Positive Allosteric Modulators

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Discovery, Structure–Activity Relationship, and Antiparkinsonian Effect of a Potent and Brain-Penetrant Chemical Series of Positive Allosteric Modulators of Metabotropic Glutamate Receptor 4

Journal of Medicinal Chemistry ◽

10.1021/acs.jmedchem.7b00991 ◽

2017 ◽

Vol 60 (20) ◽

pp. 8515-8537 ◽

Cited By ~ 19

Author(s):

Delphine Charvin ◽

Vincent Pomel ◽

Millan Ortiz ◽

Mélanie Frauli ◽

Sophie Scheffler ◽

...

Keyword(s):

Glutamate Receptor ◽

Metabotropic Glutamate Receptor ◽

Structure Activity Relationship ◽

Activity Relationship ◽

Allosteric Modulators ◽

Metabotropic Glutamate ◽

Structure Activity ◽

Positive Allosteric Modulators

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Discovery, Synthesis, and Structure−Activity Relationship Development of a Series ofN-(4-Acetamido)phenylpicolinamides as Positive Allosteric Modulators of Metabotropic Glutamate Receptor 4 (mGlu4) with CNS Exposure in Rats

Journal of Medicinal Chemistry ◽

10.1021/jm101271s ◽

2011 ◽

Vol 54 (4) ◽

pp. 1106-1110 ◽

Cited By ~ 31

Author(s):

Darren W. Engers ◽

Julie R. Field ◽

Uyen Le ◽

Ya Zhou ◽

Julie D. Bolinger ◽

...

Keyword(s):

Glutamate Receptor ◽

Metabotropic Glutamate Receptor ◽

Structure Activity Relationship ◽

Relationship Development ◽

Activity Relationship ◽

Allosteric Modulators ◽

Metabotropic Glutamate ◽

Structure Activity ◽

Positive Allosteric Modulators ◽

Cns Exposure

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Reprint of Pharmacological and molecular characterization of the positive allosteric modulators of metabotropic glutamate receptor 2

Neuropharmacology ◽

10.1016/j.neuropharm.2016.08.040 ◽

2017 ◽

Vol 115 ◽

pp. 115-127 ◽

Cited By ~ 5

Author(s):

L. Lundström ◽

C. Bissantz ◽

J. Beck ◽

M. Dellenbach ◽

T.J. Woltering ◽

...

Keyword(s):

Molecular Characterization ◽

Glutamate Receptor ◽

Metabotropic Glutamate Receptor ◽

Allosteric Modulators ◽

Metabotropic Glutamate ◽

Positive Allosteric Modulators

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Pharmacological and molecular characterization of the positive allosteric modulators of metabotropic glutamate receptor 2

Neuropharmacology ◽

10.1016/j.neuropharm.2016.08.032 ◽

2016 ◽

Vol 111 ◽

pp. 253-265 ◽

Cited By ~ 3

Author(s):

L. Lundström ◽

C. Bissantz ◽

J. Beck ◽

M. Dellenbach ◽

T.J. Woltering ◽

...

Keyword(s):

Molecular Characterization ◽

Glutamate Receptor ◽

Metabotropic Glutamate Receptor ◽

Allosteric Modulators ◽

Metabotropic Glutamate ◽

Positive Allosteric Modulators

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Discovery, Synthesis, and Structure–Activity Relationship Development of a Series ofN-4-(2,5-Dioxopyrrolidin-1-yl)phenylpicolinamides (VU0400195, ML182): Characterization of a Novel Positive Allosteric Modulator of the Metabotropic Glutamate Receptor 4 (mGlu4) with Oral Efficacy in an Antiparkinsonian Animal Model

Journal of Medicinal Chemistry ◽

10.1021/jm200956q ◽

2011 ◽

Vol 54 (21) ◽

pp. 7639-7647 ◽

Cited By ~ 40

Author(s):

Carrie K. Jones ◽

Darren W. Engers ◽

Analisa D. Thompson ◽

Julie R. Field ◽

Anna L. Blobaum ◽

...

Keyword(s):

Animal Model ◽

Glutamate Receptor ◽

Metabotropic Glutamate Receptor ◽

Relationship Development ◽

Activity Relationship ◽

Allosteric Modulator ◽

Positive Allosteric Modulator ◽

Metabotropic Glutamate ◽

Structure Activity

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

Bioorganic & Medicinal Chemistry Letters ◽

10.1016/j.bmcl.2016.05.029 ◽

2016 ◽

Vol 26 (13) ◽

pp. 2984-2987 ◽

Cited By ~ 5

Author(s):

Rocco D. Gogliotti ◽

Anna L. Blobaum ◽

Ryan M. Morrison ◽

J. Scott Daniels ◽

James M. Salovich ◽

...

Keyword(s):

Glutamate Receptor ◽

Metabotropic Glutamate Receptor ◽

Allosteric Modulators ◽

Metabotropic Glutamate ◽

Positive Allosteric Modulators

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Synthesis and Structure–Activity Relationship Studies of Novel 2-Diarylethyl Substituted (2-Carboxycycloprop-1-yl)glycines as High-Affinity Group II Metabotropic Glutamate Receptor Ligands

Bioorganic & Medicinal Chemistry ◽

10.1016/s0968-0896(02)00387-5 ◽

2003 ◽

Vol 11 (2) ◽

pp. 197-205 ◽

Cited By ~ 21

Author(s):

Ulrik S Sørensen ◽

Thomas J Bleisch ◽

Anne E Kingston ◽

Rebecca A Wright ◽

Bryan G Johnson ◽

...

Keyword(s):

Glutamate Receptor ◽

Metabotropic Glutamate Receptor ◽

Structure Activity Relationship ◽

Activity Relationship ◽

Receptor Ligands ◽

Metabotropic Glutamate ◽

High Affinity ◽

Structure Activity ◽

Affinity Group ◽

Group Ii

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Exploration of Allosteric Agonism Structure–Activity Relationships within an Acetylene Series of Metabotropic Glutamate Receptor 5 (mGlu5) Positive Allosteric Modulators (PAMs): Discovery of 5-((3-Fluorophenyl)ethynyl)-N-(3-methyloxetan-3-yl)picolinamide (ML254)

Journal of Medicinal Chemistry ◽

10.1021/jm401028t ◽

2013 ◽

Vol 56 (20) ◽

pp. 7976-7996 ◽

Cited By ~ 24

Author(s):

Mark Turlington ◽

Meredith J. Noetzel ◽

Aspen Chun ◽

Ya Zhou ◽

Rocco D. Gogliotti ◽

...

Keyword(s):

Glutamate Receptor ◽

Metabotropic Glutamate Receptor ◽

Allosteric Modulators ◽

Metabotropic Glutamate Receptor 5 ◽

Structure Activity Relationships ◽

Metabotropic Glutamate ◽

Acetylene Series ◽

Structure Activity ◽

Positive Allosteric Modulators

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Exploring the Active Conformation of Cyclohexane Carboxylate Positive Allosteric Modulators of the Type 4 Metabotropic Glutamate Receptor

ChemMedChem ◽

10.1002/cmdc.201402190 ◽

2014 ◽

Vol 9 (12) ◽

pp. 2685-2698 ◽

Cited By ~ 1

Author(s):

Xavier Rovira ◽

Youssef Harrak ◽

Ana Trapero ◽

Patricia González-Bulnes ◽

Fanny Malhaire ◽

...

Keyword(s):

Glutamate Receptor ◽

Metabotropic Glutamate Receptor ◽

Allosteric Modulators ◽

Active Conformation ◽

Metabotropic Glutamate ◽

Cyclohexane Carboxylate ◽

Positive Allosteric Modulators

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Identification and optimisation of a series of tetrahydrobenzotriazoles as metabotropic glutamate receptor 5-selective positive allosteric modulators that improve performance in a preclinical model of cognition

Bioorganic & Medicinal Chemistry Letters ◽

10.1016/j.bmcl.2015.10.050 ◽

2015 ◽

Vol 25 (24) ◽

pp. 5792-5796 ◽

Cited By ~ 5

Author(s):

John M. Ellard ◽

Andrew Madin ◽

Oliver Philps ◽

Mark Hopkin ◽

Scott Henderson ◽

...

Keyword(s):

Glutamate Receptor ◽

Metabotropic Glutamate Receptor ◽

Preclinical Model ◽

Allosteric Modulators ◽

Improve Performance ◽

Metabotropic Glutamate Receptor 5 ◽

Metabotropic Glutamate ◽

Positive Allosteric Modulators

Download Full-text