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

Allosteric Regulation Amides / chemistry Animals Brain / metabolism Catalepsy / chemically induced Cytochrome P-450 CYP1A2 / metabolism Half-Life Haloperidol / toxicity Humans Isoxazoles / chemistry Male Rats Rats, Sprague-Dawley Receptors, Metabotropic Glutamate / chemistry Structure-Activity Relationship

Journal

Journal of medicinal chemistry
ISSN: 1520-4804
Titre abrégé: J Med Chem
Pays: United States
ID NLM: 9716531

Informations de publication

Date de publication:
10 01 2019
Historique:
pubmed: 25 9 2018
medline: 15 10 2019
entrez: 25 9 2018
Statut: ppublish

Résumé

This work describes the discovery and characterization of novel 6-(1 H-pyrazolo[4,3- b]pyridin-3-yl)amino-benzo[ d]isothiazole-3-carboxamides as mGlu

Identifiants

DOI: 10.1021/acs.jmedchem.8b00994 PMID: 30247901
pubmed: 30247901
doi: 10.1021/acs.jmedchem.8b00994
doi:

Substances chimiques

Amides 0
Isoxazoles 0
Receptors, Metabotropic Glutamate 0
Cytochrome P-450 CYP1A2 EC 1.14.14.1
Haloperidol J6292F8L3D
metabotropic glutamate receptor 4 YZN9W7P1BX

Types de publication

Journal Article Research Support, Non-U.S. Gov't

Langues

eng

Sous-ensembles de citation

IM

Pagination

342-358

Auteurs

Sean R Bollinger (SR)

Vanderbilt Center for Neuroscience Drug Discovery , Vanderbilt University , Nashville , Tennessee 37232 , United States.
Department of Pharmacology , Vanderbilt University , Nashville , Tennessee 37232 , United States.

Darren W Engers (DW)

Vanderbilt Center for Neuroscience Drug Discovery , Vanderbilt University , Nashville , Tennessee 37232 , United States.
Department of Pharmacology , Vanderbilt University , Nashville , Tennessee 37232 , United States.

Joseph D Panarese (JD)

Vanderbilt Center for Neuroscience Drug Discovery , Vanderbilt University , Nashville , Tennessee 37232 , United States.
Department of Pharmacology , Vanderbilt University , Nashville , Tennessee 37232 , United States.

Mary West (M)

Vanderbilt Center for Neuroscience Drug Discovery , Vanderbilt University , Nashville , Tennessee 37232 , United States.
Department of Pharmacology , Vanderbilt University , Nashville , Tennessee 37232 , United States.

Julie L Engers (JL)

Vanderbilt Center for Neuroscience Drug Discovery , Vanderbilt University , Nashville , Tennessee 37232 , United States.
Department of Pharmacology , Vanderbilt University , Nashville , Tennessee 37232 , United States.

Matthew T Loch (MT)

Vanderbilt Center for Neuroscience Drug Discovery , Vanderbilt University , Nashville , Tennessee 37232 , United States.
Department of Pharmacology , Vanderbilt University , Nashville , Tennessee 37232 , United States.

Alice L Rodriguez (AL)

Vanderbilt Center for Neuroscience Drug Discovery , Vanderbilt University , Nashville , Tennessee 37232 , United States.
Department of Pharmacology , Vanderbilt University , Nashville , Tennessee 37232 , United States.

Anna L Blobaum (AL)

Vanderbilt Center for Neuroscience Drug Discovery , Vanderbilt University , Nashville , Tennessee 37232 , United States.
Department of Pharmacology , Vanderbilt University , Nashville , Tennessee 37232 , United States.

Carrie K Jones (CK)

Vanderbilt Center for Neuroscience Drug Discovery , Vanderbilt University , Nashville , Tennessee 37232 , United States.
Department of Pharmacology , Vanderbilt University , Nashville , Tennessee 37232 , United States.

Analisa Thompson Gray (A)

Vanderbilt Center for Neuroscience Drug Discovery , Vanderbilt University , Nashville , Tennessee 37232 , United States.
Department of Pharmacology , Vanderbilt University , Nashville , Tennessee 37232 , United States.

P Jeffrey Conn (PJ)

Vanderbilt Center for Neuroscience Drug Discovery , Vanderbilt University , Nashville , Tennessee 37232 , United States.
Department of Pharmacology , Vanderbilt University , Nashville , Tennessee 37232 , United States.
Vanderbilt Kennedy Center , Vanderbilt University Medical Center , Nashville , Tennessee 37232 , United States.

Craig W Lindsley (CW)

Vanderbilt Center for Neuroscience Drug Discovery , Vanderbilt University , Nashville , Tennessee 37232 , United States.
Department of Pharmacology , Vanderbilt University , Nashville , Tennessee 37232 , United States.
Department of Chemistry , Vanderbilt University , Nashville , Tennessee 37232 , United States.
Department of Biochemistry , Vanderbilt University , Nashville , Tennessee 37232 , United States.
ORCID: 0000-0003-0168-1445

Colleen M Niswender (CM)

Vanderbilt Center for Neuroscience Drug Discovery , Vanderbilt University , Nashville , Tennessee 37232 , United States.
Department of Pharmacology , Vanderbilt University , Nashville , Tennessee 37232 , United States.
Vanderbilt Kennedy Center , Vanderbilt University Medical Center , Nashville , Tennessee 37232 , United States.

Corey R Hopkins (CR)

Vanderbilt Center for Neuroscience Drug Discovery , Vanderbilt University , Nashville , Tennessee 37232 , United States.
Department of Pharmacology , Vanderbilt University , Nashville , Tennessee 37232 , United States.
Department of Chemistry , Vanderbilt University , Nashville , Tennessee 37232 , United States.
ORCID: 0000-0003-4958-1697

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Classifications MeSH

questionsmedicales.fr › Phénomènes chimiques › Phénomènes biochimiques › Régulation allostérique › Discovery, Structure-Activity Relationship,...
questionsmedicales.fr › Composés chimiques organiques › Amides › Discovery, Structure-Activity Relationship,...
questionsmedicales.fr › Eucaryotes › Animaux › Discovery, Structure-Activity Relationship,...
questionsmedicales.fr › Système nerveux › Système nerveux central › Encéphale › Discovery, Structure-Activity Relationship,...
questionsmedicales.fr › États, signes et symptômes pathologiques › Signes et symptômes › Manifestations neurologiques › Dyskinésies › Catalepsie › Discovery, Structure-Activity Relationship,...
questionsmedicales.fr › Acides aminés, peptides et protéines › Protéines › Hémoprotéines › Cytochromes › Cytochrome P-450 enzyme system › Famille-1 de cytochromes P450 › Cytochrome P-450 CYP1A2 › Discovery, Structure-Activity Relationship,...
questionsmedicales.fr › Phénomènes physiques › Temps › Période › Discovery, Structure-Activity Relationship,...
questionsmedicales.fr › Composés chimiques organiques › Cétones › Butyrophénones › Halopéridol › Discovery, Structure-Activity Relationship,...
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Primates › Haplorhini › Catarrhini › Hominidae › Humains › Discovery, Structure-Activity Relationship,...
questionsmedicales.fr › Composés hétérocycliques › Composés hétéromonocycliques › Azoles › Isoxazoles › Discovery, Structure-Activity Relationship,...
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Rodentia › Muridae › Murinae › Rats › Discovery, Structure-Activity Relationship,...
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Rodentia › Muridae › Murinae › Rats › Rat Sprague-Dawley › Discovery, Structure-Activity Relationship,...
questionsmedicales.fr › Acides aminés, peptides et protéines › Protéines › Protéines membranaires › Récepteurs de surface cellulaire › Récepteurs aux neuromédiateurs › Récepteurs aux acides aminés › Récepteurs au glutamate › Récepteurs métabotropes au glutamate › Discovery, Structure-Activity Relationship,...
questionsmedicales.fr › Phénomènes physiologiques › Phénomènes pharmacologiques et toxicologiques › Phénomènes pharmacologiques › Relation structure-activité › Discovery, Structure-Activity Relationship,...