Design, Synthesis, and Evaluation of

Animals Brain / diagnostic imaging Carbon Radioisotopes / chemistry Diacylglycerol Kinase / metabolism Drug Design Humans Indoles / chemical synthesis Male Mice, Inbred C57BL Positron-Emission Tomography Radiopharmaceuticals / chemical synthesis Rats, Sprague-Dawley

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:
26 08 2021
Historique:
pubmed: 5 8 2021
medline: 16 11 2021
entrez: 4 8 2021
Statut: ppublish

Résumé

Diacylglycerol kinase gamma (DGKγ) is a subtype of DGK enzyme, which catalyzes ATP-dependent conversion of diacylglycerol to phosphatidic acid. DGKγ, localized in the brain, plays an important role in the central nervous system. However, its function has not been widely investigated. Positron emission tomography (PET) imaging of DGKγ validates target engagement of therapeutic DGKγ inhibitors and investigates DGKγ levels under normal and disease conditions. In this study, we designed and synthesized a series of 3-acetyl indole derivatives as candidates for PET imaging agents for DGKγ. Among the synthesized compounds, 2-((3-acetyl-1-(6-methoxypyridin-3-yl)-2-methyl-1H-indol-5-yl)oxy)-N-methylacetamide (

Identifiants

DOI: 10.1021/acs.jmedchem.1c00584 PMID: 34347478
pubmed: 34347478
doi: 10.1021/acs.jmedchem.1c00584
doi:

Substances chimiques

Carbon Radioisotopes 0
Carbon-11 0
Indoles 0
Radiopharmaceuticals 0
Diacylglycerol Kinase EC 2.7.1.107

Types de publication

Journal Article

Langues

eng

Sous-ensembles de citation

IM

Pagination

11990-12002

Auteurs

Yasushi Hattori (Y)

Takeda Pharmaceutical Company Limited, 26-1 Muraoka-Higashi, 2-Chome, Fujisawa, Kanagawa 251-8555, Japan.
ORCID: 0000-0003-4054-3619

Tomoteru Yamasaki (T)

Department of Advanced Nuclear Medicine Sciences, National Institute of Radiological Sciences, National Institutes for Quantum and Radiological Science and Technology, 4-9-1, Anagawa, Inage-ku, Chiba 263-8555, Japan.

Tomohiro Ohashi (T)

Takeda Pharmaceutical Company Limited, 26-1 Muraoka-Higashi, 2-Chome, Fujisawa, Kanagawa 251-8555, Japan.

Yuhei Miyanohana (Y)

Takeda Pharmaceutical Company Limited, 26-1 Muraoka-Higashi, 2-Chome, Fujisawa, Kanagawa 251-8555, Japan.

Tomokazu Kusumoto (T)

Takeda Pharmaceutical Company Limited, 26-1 Muraoka-Higashi, 2-Chome, Fujisawa, Kanagawa 251-8555, Japan.

Ryouta Maeda (R)

Takeda Pharmaceutical Company Limited, 26-1 Muraoka-Higashi, 2-Chome, Fujisawa, Kanagawa 251-8555, Japan.

Maki Miyamoto (M)

Takeda Pharmaceutical Company Limited, 26-1 Muraoka-Higashi, 2-Chome, Fujisawa, Kanagawa 251-8555, Japan.

Yasuyuki Debori (Y)

Takeda Pharmaceutical Company Limited, 26-1 Muraoka-Higashi, 2-Chome, Fujisawa, Kanagawa 251-8555, Japan.

Akito Hata (A)

Takeda Pharmaceutical Company Limited, 26-1 Muraoka-Higashi, 2-Chome, Fujisawa, Kanagawa 251-8555, Japan.

Yiding Zhang (Y)

Department of Advanced Nuclear Medicine Sciences, National Institute of Radiological Sciences, National Institutes for Quantum and Radiological Science and Technology, 4-9-1, Anagawa, Inage-ku, Chiba 263-8555, Japan.

Hidekatsu Wakizaka (H)

Department of Advanced Nuclear Medicine Sciences, National Institute of Radiological Sciences, National Institutes for Quantum and Radiological Science and Technology, 4-9-1, Anagawa, Inage-ku, Chiba 263-8555, Japan.

Takeshi Wakabayashi (T)

Takeda Pharmaceutical Company Limited, 26-1 Muraoka-Higashi, 2-Chome, Fujisawa, Kanagawa 251-8555, Japan.

Masayuki Fujinaga (M)

Department of Advanced Nuclear Medicine Sciences, National Institute of Radiological Sciences, National Institutes for Quantum and Radiological Science and Technology, 4-9-1, Anagawa, Inage-ku, Chiba 263-8555, Japan.

Ryo Yamashita (R)

Takeda Pharmaceutical Company Limited, 26-1 Muraoka-Higashi, 2-Chome, Fujisawa, Kanagawa 251-8555, Japan.

Ming-Rong Zhang (MR)

Department of Advanced Nuclear Medicine Sciences, National Institute of Radiological Sciences, National Institutes for Quantum and Radiological Science and Technology, 4-9-1, Anagawa, Inage-ku, Chiba 263-8555, Japan.

Tatsuki Koike (T)

Takeda Pharmaceutical Company Limited, 26-1 Muraoka-Higashi, 2-Chome, Fujisawa, Kanagawa 251-8555, Japan.
ORCID: 0000-0002-3264-1406

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Classifications MeSH

questionsmedicales.fr › Eucaryotes › Animaux › Design, Synthesis, and Evaluation of
questionsmedicales.fr › Système nerveux › Système nerveux central › Encéphale › Design, Synthesis, and Evaluation of
questionsmedicales.fr › Produits chimiques inorganiques › Isotopes › Radio-isotopes › Radio-isotopes du carbone › Design, Synthesis, and Evaluation of
questionsmedicales.fr › Enzymes et coenzymes › Enzymes › Transferases › Phosphotransferases › Phosphotransferases (Alcohol Group Acceptor) › Diacylglycérol kinase › Design, Synthesis, and Evaluation of
questionsmedicales.fr › Techniques d'investigation › Développement de médicament › Découverte de médicament › Conception de médicament › Design, Synthesis, and Evaluation of
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Primates › Haplorhini › Catarrhini › Hominidae › Humains › Design, Synthesis, and Evaluation of
questionsmedicales.fr › Composés hétérocycliques › Composés hétérocycliques à cycles fusionnés › Composés hétérobicycliques › Indoles › Design, Synthesis, and Evaluation of
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Rodentia › Muridae › Murinae › Souris › Lignées consanguines de souris › Souris de lignée C57BL › Design, Synthesis, and Evaluation of
questionsmedicales.fr › Diagnostic › Techniques et procédures diagnostiques › Techniques de diagnostic radioisotopique › Scintigraphie › Tomoscintigraphie › Tomographie par émission de positons › Design, Synthesis, and Evaluation of
questionsmedicales.fr › Actions chimiques et utilisations › Utilisations spécialisées de produits chimiques › Produits chimiques de laboratoire › Indicateurs et réactifs › Radiopharmaceutiques › Design, Synthesis, and Evaluation of
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Rodentia › Muridae › Murinae › Rats › Rat Sprague-Dawley › Design, Synthesis, and Evaluation of