Discovery and Development of S6821 and S7958 as Potent TAS2R8 Antagonists.
Animals
Coffee
/ chemistry
Drug Discovery
Drug Stability
Humans
Hydantoins
/ chemical synthesis
Molecular Structure
Pyrazoles
/ chemical synthesis
Rats
Receptors, Cell Surface
/ antagonists & inhibitors
Receptors, G-Protein-Coupled
/ antagonists & inhibitors
Structure-Activity Relationship
Taste
/ drug effects
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:
14 05 2020
14 05 2020
Historique:
pubmed:
25
4
2020
medline:
3
11
2020
entrez:
25
4
2020
Statut:
ppublish
Résumé
In humans, bitter taste is mediated by 25 TAS2Rs. Many compounds, including certain active pharmaceutical ingredients, excipients, and nutraceuticals, impart their bitter taste (or in part) through TAS2R8 activation. However, effective TAS2R8 blockers that can either suppress or reduce the bitterness of these compounds have not been described. We are hereby reporting a series of novel 3-(pyrazol-4-yl) imidazolidine-2,4-diones as potent and selective TAS2R8 antagonists. In human sensory tests,
Identifiants
pubmed: 32330040
doi: 10.1021/acs.jmedchem.0c00388
doi:
Substances chimiques
Coffee
0
Hydantoins
0
Pyrazoles
0
Receptors, Cell Surface
0
Receptors, G-Protein-Coupled
0
TAS2R8 protein, human
0
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM