Discovery of 2-Aminopyrimidines as Potent Agonists for the Bitter Taste Receptor TAS2R14.

Humans Taste Flufenamic Acid Receptors, G-Protein-Coupled / agonists Muscle, Smooth

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:
09 03 2023
Historique:
pubmed: 28 2 2023
medline: 11 3 2023
entrez: 27 2 2023
Statut: ppublish

Résumé

The bitter taste receptor TAS2R14 is a G protein-coupled receptor that is found on the tongue as well as in the human airway smooth muscle and other extraoral tissues. Because its activation causes bronchodilatation, TAS2R14 is a potential target for the treatment of asthma or chronic obstructive pulmonary disease. Structural variations of flufenamic acid, a nonsteroidal anti-inflammatory drug, led us to 2-aminopyridines showing considerable efficacy and potency in an IP

Identifiants

DOI: 10.1021/acs.jmedchem.2c01997 PMID: 36847646
pubmed: 36847646
doi: 10.1021/acs.jmedchem.2c01997
doi:

Substances chimiques

2-aminopyrimidine 109-12-6
Flufenamic Acid 60GCX7Y6BH
Receptors, G-Protein-Coupled 0

Types de publication

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

Langues

eng

Sous-ensembles de citation

IM

Pagination

3499-3521

Auteurs

Lukas Waterloo (L)

Department of Chemistry and Pharmacy, Medicinal Chemistry, Friedrich-Alexander-Universität Erlangen-Nürnberg, Nikolaus-Fiebiger-Str. 10, Erlangen 91058, Germany.

Harald Hübner (H)

Department of Chemistry and Pharmacy, Medicinal Chemistry, Friedrich-Alexander-Universität Erlangen-Nürnberg, Nikolaus-Fiebiger-Str. 10, Erlangen 91058, Germany.

Fabrizio Fierro (F)

The Robert H. Smith Faculty of Agriculture, Food and Environment, Institute of Biochemistry, Food Science and Nutrition, The Hebrew University, Rehovot 7610001, Israel.

Tara Pfeiffer (T)

Department of Chemistry and Pharmacy, Medicinal Chemistry, Friedrich-Alexander-Universität Erlangen-Nürnberg, Nikolaus-Fiebiger-Str. 10, Erlangen 91058, Germany.
ORCID: 0000-0003-1701-0996

Regine Brox (R)

Department of Chemistry and Pharmacy, Medicinal Chemistry, Friedrich-Alexander-Universität Erlangen-Nürnberg, Nikolaus-Fiebiger-Str. 10, Erlangen 91058, Germany.

Stefan Löber (S)

Department of Chemistry and Pharmacy, Medicinal Chemistry, Friedrich-Alexander-Universität Erlangen-Nürnberg, Nikolaus-Fiebiger-Str. 10, Erlangen 91058, Germany.

Dorothee Weikert (D)

Department of Chemistry and Pharmacy, Medicinal Chemistry, Friedrich-Alexander-Universität Erlangen-Nürnberg, Nikolaus-Fiebiger-Str. 10, Erlangen 91058, Germany.
ORCID: 0000-0003-2259-9002

Masha Y Niv (MY)

The Robert H. Smith Faculty of Agriculture, Food and Environment, Institute of Biochemistry, Food Science and Nutrition, The Hebrew University, Rehovot 7610001, Israel.

Peter Gmeiner (P)

Department of Chemistry and Pharmacy, Medicinal Chemistry, Friedrich-Alexander-Universität Erlangen-Nürnberg, Nikolaus-Fiebiger-Str. 10, Erlangen 91058, Germany.
ORCID: 0000-0002-4127-197X

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Classifications MeSH

questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Primates › Haplorhini › Catarrhini › Hominidae › Humains › Discovery of 2-Aminopyrimidines as Potent...
questionsmedicales.fr › Phénomènes physiologiques de l'appareil locomoteur et du système nerveux › Phénomènes physiologiques du système nerveux › Sensation › Goût › Discovery of 2-Aminopyrimidines as Potent...
questionsmedicales.fr › Composés chimiques organiques › Hydrocarbures › Hydrocarbures cycliques › Hydrocarbures aromatiques › Dérivés du benzène › Benzoates › Aminobenzoates › ortho-Aminobenzoates › Fénamates › Acide flufénamique › Discovery of 2-Aminopyrimidines as Potent...
questionsmedicales.fr › Acides aminés, peptides et protéines › Protéines › Protéines membranaires › Récepteurs de surface cellulaire › Récepteurs couplés aux protéines G › Discovery of 2-Aminopyrimidines as Potent...
questionsmedicales.fr › Tissus › Muscles › Muscles lisses › Discovery of 2-Aminopyrimidines as Potent...