Synthesis and characterization of chiral 6-azaspiro[2.5]octanes as potent and selective antagonists of the M

Dose-Response Relationship, Drug Humans Molecular Structure Muscarinic Antagonists / chemical synthesis Receptor, Muscarinic M4 / antagonists & inhibitors Structure-Activity Relationship
Deuterium SAR Spirocycle cytochrome P450 muscarinic acetylcholine receptor M(4)

Journal

Bioorganic & medicinal chemistry letters
ISSN: 1464-3405
Titre abrégé: Bioorg Med Chem Lett
Pays: England
ID NLM: 9107377

Informations de publication

Date de publication:
15 01 2022
Historique:
received: 05 08 2021
revised: 11 11 2021
accepted: 20 11 2021
pubmed: 29 11 2021
medline: 23 2 2022
entrez: 28 11 2021
Statut: ppublish

Résumé

In this manuscript, we report a series of chiral 6-azaspiro[2.5]octanes and related spirocycles as highly potent and selective antagonists of the muscarinic acetylcholine receptor subtype 4 (mAChR

Identifiants

DOI: 10.1016/j.bmcl.2021.128479 PMID: 34838649
pubmed: 34838649
pii: S0960-894X(21)00706-X
doi: 10.1016/j.bmcl.2021.128479
pii:
doi:

Substances chimiques

Muscarinic Antagonists 0
Receptor, Muscarinic M4 0

Types de publication

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

Langues

eng

Sous-ensembles de citation

IM

Pagination

128479

Informations de copyright

Copyright © 2021 Elsevier Ltd. All rights reserved.

Auteurs

Aaron M Bender (AM)

Warren Center for Neuroscience Drug Discovery, Vanderbilt University Medical Center, Nashville, TN 37232, United States; Department of Pharmacology, Vanderbilt University Medical Center, Nashville, TN 37232, United States. Electronic address: aaron.bender@vanderbilt.edu.

Trever R Carter (TR)

Warren Center for Neuroscience Drug Discovery, Vanderbilt University Medical Center, Nashville, TN 37232, United States; Department of Pharmacology, Vanderbilt University Medical Center, Nashville, TN 37232, United States.

Matthew Spock (M)

Warren Center for Neuroscience Drug Discovery, Vanderbilt University Medical Center, Nashville, TN 37232, United States; Department of Pharmacology, Vanderbilt University Medical Center, Nashville, TN 37232, United States.

Alice L Rodriguez (AL)

Warren Center for Neuroscience Drug Discovery, Vanderbilt University Medical Center, Nashville, TN 37232, United States; Department of Pharmacology, Vanderbilt University Medical Center, Nashville, TN 37232, United States.

Jonathan W Dickerson (JW)

Warren Center for Neuroscience Drug Discovery, Vanderbilt University Medical Center, Nashville, TN 37232, United States; Department of Pharmacology, Vanderbilt University Medical Center, Nashville, TN 37232, United States.

Jerri M Rook (JM)

Warren Center for Neuroscience Drug Discovery, Vanderbilt University Medical Center, Nashville, TN 37232, United States; Department of Pharmacology, Vanderbilt University Medical Center, Nashville, TN 37232, United States.

Sichen Chang (S)

Warren Center for Neuroscience Drug Discovery, Vanderbilt University Medical Center, Nashville, TN 37232, United States; Department of Pharmacology, Vanderbilt University Medical Center, Nashville, TN 37232, United States.

Aidong Qi (A)

Warren Center for Neuroscience Drug Discovery, Vanderbilt University Medical Center, Nashville, TN 37232, United States; Department of Pharmacology, Vanderbilt University Medical Center, Nashville, TN 37232, United States.

Christopher C Presley (CC)

Warren Center for Neuroscience Drug Discovery, Vanderbilt University Medical Center, Nashville, TN 37232, United States; Department of Pharmacology, Vanderbilt University Medical Center, Nashville, TN 37232, United States.

Darren W Engers (DW)

Warren Center for Neuroscience Drug Discovery, Vanderbilt University Medical Center, Nashville, TN 37232, United States; Department of Pharmacology, Vanderbilt University Medical Center, Nashville, TN 37232, United States.

Joel M Harp (JM)

Department of Biochemistry, Vanderbilt University Medical Center, Nashville, TN 37232, United States.

Thomas M Bridges (TM)

Warren Center for Neuroscience Drug Discovery, Vanderbilt University Medical Center, Nashville, TN 37232, United States; Department of Pharmacology, Vanderbilt University Medical Center, Nashville, TN 37232, United States.

Colleen M Niswender (CM)

Warren Center for Neuroscience Drug Discovery, Vanderbilt University Medical Center, Nashville, TN 37232, United States; Department of Pharmacology, Vanderbilt University Medical Center, Nashville, TN 37232, United States; Vanderbilt Kennedy Center, Vanderbilt University Medical Center, Nashville, TN 37232, United States; Vanderbilt Brain Institute, Vanderbilt University School of Medicine, Nashville, TN 37232, USA; Vanderbilt Institute of Chemical Biology, Vanderbilt University School of Medicine, Nashville, TN 37232, USA.

P Jeffrey Conn (PJ)

Warren Center for Neuroscience Drug Discovery, Vanderbilt University Medical Center, Nashville, TN 37232, United States; Department of Pharmacology, Vanderbilt University Medical Center, Nashville, TN 37232, United States; Vanderbilt Kennedy Center, Vanderbilt University Medical Center, Nashville, TN 37232, United States; Vanderbilt Brain Institute, Vanderbilt University School of Medicine, Nashville, TN 37232, USA; Vanderbilt Institute of Chemical Biology, Vanderbilt University School of Medicine, Nashville, TN 37232, USA.

Craig W Lindsley (CW)

Warren Center for Neuroscience Drug Discovery, Vanderbilt University Medical Center, Nashville, TN 37232, United States; Department of Pharmacology, Vanderbilt University Medical Center, Nashville, TN 37232, United States; Department of Chemistry, Vanderbilt University Medical Center, Nashville, TN 37232, United States; Department of Biochemistry, Vanderbilt University Medical Center, Nashville, TN 37232, United States. Electronic address: craig.lindsley@vanderbilt.edu.

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Classifications MeSH

questionsmedicales.fr › Phénomènes physiologiques › Phénomènes pharmacologiques et toxicologiques › Phénomènes toxicologiques › Relation dose-effet des médicaments › Synthesis and characterization of chiral...
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Primates › Haplorhini › Catarrhini › Hominidae › Humains › Synthesis and characterization of chiral...
questionsmedicales.fr › Phénomènes chimiques › Structure moléculaire › Synthesis and characterization of chiral...
questionsmedicales.fr › Actions chimiques et utilisations › Actions pharmacologiques › Effets physiologiques des médicaments › Agents neuromédiateurs › Agents cholinergiques › Antagonistes cholinergiques › Antagonistes muscariniques › Synthesis and characterization of chiral...
questionsmedicales.fr › Acides aminés, peptides et protéines › Protéines › Protéines membranaires › Récepteurs de surface cellulaire › Récepteurs aux neuromédiateurs › Récepteurs cholinergiques › Récepteur muscarinique › Récepteur muscarinique de type M4 › Synthesis and characterization of chiral...
questionsmedicales.fr › Phénomènes physiologiques › Phénomènes pharmacologiques et toxicologiques › Phénomènes pharmacologiques › Relation structure-activité › Synthesis and characterization of chiral...