Discovery of a Series of Pyrimidine Carboxamides as Inhibitors of Vanin-1.

Amidohydrolases / antagonists & inhibitors Animals Colitis / chemically induced Crystallography, X-Ray Dextran Sulfate Dogs Drug Discovery Female GPI-Linked Proteins / antagonists & inhibitors High-Throughput Screening Assays Ketones / chemistry Mice Mice, Inbred BALB C Models, Molecular Pyridines / chemical synthesis Rats 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:
13 01 2022
Historique:
pubmed: 31 12 2021
medline: 8 2 2022
entrez: 30 12 2021
Statut: ppublish

Résumé

A diaryl ketone series was identified as vanin-1 inhibitors from a high-throughput screening campaign. While this novel scaffold provided valuable probe

Identifiants

DOI: 10.1021/acs.jmedchem.1c01849 PMID: 34967602
pubmed: 34967602
doi: 10.1021/acs.jmedchem.1c01849
doi:

Substances chimiques

GPI-Linked Proteins 0
Ketones 0
Pyridines 0
Dextran Sulfate 9042-14-2
Amidohydrolases EC 3.5.-
pantetheinase EC 3.5.1.-

Types de publication

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

Langues

eng

Sous-ensembles de citation

IM

Pagination

757-784

Auteurs

Agustin Casimiro-Garcia (A)

Medicine Design, Pfizer Inc., 1 Portland Street, Cambridge, Massachusetts 02139, United States.
ORCID: 0000-0001-9618-2547

Christophe Allais (C)

Medicine Design, Pfizer Inc., 445 Eastern Point Rd, Groton, Connecticut 06340, United States.
ORCID: 0000-0002-3443-9391

Agnes Brennan (A)

Inflammation and Immunology Research Unit, Pfizer Inc., 1 Portland Street, Cambridge, Massachusetts 02139, United States.

Chulho Choi (C)

Medicine Design, Pfizer Inc., 445 Eastern Point Rd, Groton, Connecticut 06340, United States.
ORCID: 0000-0003-3459-3767

Gabriela Dower (G)

Inflammation and Immunology Research Unit, Pfizer Inc., 1 Portland Street, Cambridge, Massachusetts 02139, United States.

Kathleen A Farley (KA)

Medicine Design, Pfizer Inc., 445 Eastern Point Rd, Groton, Connecticut 06340, United States.
ORCID: 0000-0001-8935-6852

Margaret Fleming (M)

Inflammation and Immunology Research Unit, Pfizer Inc., 1 Portland Street, Cambridge, Massachusetts 02139, United States.

Andrew Flick (A)

Medicine Design, Pfizer Inc., 445 Eastern Point Rd, Groton, Connecticut 06340, United States.

Richard K Frisbie (RK)

Medicine Design, Pfizer Inc., 445 Eastern Point Rd, Groton, Connecticut 06340, United States.

Justin Hall (J)

Medicine Design, Pfizer Inc., 445 Eastern Point Rd, Groton, Connecticut 06340, United States.

David Hepworth (D)

Medicine Design, Pfizer Inc., 1 Portland Street, Cambridge, Massachusetts 02139, United States.

Hannah Jones (H)

Medicine Design, Pfizer Inc., 1 Portland Street, Cambridge, Massachusetts 02139, United States.

John D Knafels (JD)

Medicine Design, Pfizer Inc., 445 Eastern Point Rd, Groton, Connecticut 06340, United States.

Steve Kortum (S)

Medicine Design, Pfizer Inc., 445 Eastern Point Rd, Groton, Connecticut 06340, United States.

Frank E Lovering (FE)

Medicine Design, Pfizer Inc., 1 Portland Street, Cambridge, Massachusetts 02139, United States.

John P Mathias (JP)

Medicine Design, Pfizer Inc., 1 Portland Street, Cambridge, Massachusetts 02139, United States.

Sashi Mohan (S)

Inflammation and Immunology Research Unit, Pfizer Inc., 1 Portland Street, Cambridge, Massachusetts 02139, United States.

Paul M Morgan (PM)

Inflammation and Immunology Research Unit, Pfizer Inc., 1 Portland Street, Cambridge, Massachusetts 02139, United States.

Chuenlei Parng (C)

Medicine Design, Pfizer Inc., 1 Portland Street, Cambridge, Massachusetts 02139, United States.

Kevin Parris (K)

Medicine Design, Pfizer Inc., 445 Eastern Point Rd, Groton, Connecticut 06340, United States.

Nick Pullen (N)

Inflammation and Immunology Research Unit, Pfizer Inc., 1 Portland Street, Cambridge, Massachusetts 02139, United States.

Franklin Schlerman (F)

Inflammation and Immunology Research Unit, Pfizer Inc., 1 Portland Street, Cambridge, Massachusetts 02139, United States.

John Stansfield (J)

Early Clinical Development Non-Clinical Statistics, Pfizer Inc., 1 Portland Street, Cambridge, Massachusetts 02139, United States.

Joseph W Strohbach (JW)

Medicine Design, Pfizer Inc., 1 Portland Street, Cambridge, Massachusetts 02139, United States.

Felix F Vajdos (FF)

Medicine Design, Pfizer Inc., 445 Eastern Point Rd, Groton, Connecticut 06340, United States.

Fabien Vincent (F)

Medicine Design, Pfizer Inc., 445 Eastern Point Rd, Groton, Connecticut 06340, United States.

Hong Wang (H)

Medicine Design, Pfizer Inc., 445 Eastern Point Rd, Groton, Connecticut 06340, United States.

Xiaolun Wang (X)

Medicine Design, Pfizer Inc., 1 Portland Street, Cambridge, Massachusetts 02139, United States.
ORCID: 0000-0001-9576-7746

Robert Webster (R)

Medicine Design, Pfizer Inc., 1 Portland Street, Cambridge, Massachusetts 02139, United States.

Stephen W Wright (SW)

Medicine Design, Pfizer Inc., 445 Eastern Point Rd, Groton, Connecticut 06340, United States.

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Classifications MeSH

questionsmedicales.fr › Enzymes et coenzymes › Enzymes › Hydrolases › Amidohydrolases › Discovery of a Series of Pyrimidine...
questionsmedicales.fr › Eucaryotes › Animaux › Discovery of a Series of Pyrimidine...
questionsmedicales.fr › Maladies de l'appareil digestif › Maladies gastro-intestinales › Maladies intestinales › Maladies du côlon › Colite › Discovery of a Series of Pyrimidine...
questionsmedicales.fr › Techniques d'investigation › Techniques de chimie analytique › Cristallographie aux rayons X › Discovery of a Series of Pyrimidine...
questionsmedicales.fr › Glucides › Polyosides › Glucanes › Dextrane › Sulfate dextran › Discovery of a Series of Pyrimidine...
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Carnivora › Pinnipedia › Canidae › Chiens › Discovery of a Series of Pyrimidine...
questionsmedicales.fr › Techniques d'investigation › Développement de médicament › Découverte de médicament › Discovery of a Series of Pyrimidine...
questionsmedicales.fr › Acides aminés, peptides et protéines › Protéines › Protéines membranaires › Glycoprotéines membranaires › Protéines liées au GPI › Discovery of a Series of Pyrimidine...
questionsmedicales.fr › Techniques d'investigation › Tests de criblage à haut débit › Discovery of a Series of Pyrimidine...
questionsmedicales.fr › Composés chimiques organiques › Cétones › Discovery of a Series of Pyrimidine...
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Rodentia › Muridae › Murinae › Souris › Discovery of a Series of Pyrimidine...
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Rodentia › Muridae › Murinae › Souris › Lignées consanguines de souris › Souris de lignée BALB C › Discovery of a Series of Pyrimidine...
questionsmedicales.fr › Techniques d'investigation › Modèles théoriques › Modèles moléculaires › Discovery of a Series of Pyrimidine...
questionsmedicales.fr › Composés hétérocycliques › Composés hétéromonocycliques › Pyridines › Discovery of a Series of Pyrimidine...
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Rodentia › Muridae › Murinae › Rats › Discovery of a Series of Pyrimidine...
questionsmedicales.fr › Phénomènes physiologiques › Phénomènes pharmacologiques et toxicologiques › Phénomènes pharmacologiques › Relation structure-activité › Discovery of a Series of Pyrimidine...