Effect of 6-Benzoyl-benzothiazol-2-one scaffold on the pharmacological profile of α-alkoxyphenylpropionic acid derived PPAR agonists.
Animals
Benzothiazoles
/ chemical synthesis
COS Cells
Chlorocebus aethiops
Diabetes Mellitus, Type 2
/ drug therapy
Dose-Response Relationship, Drug
Hypoglycemic Agents
/ chemical synthesis
Ligands
Male
Mice
Mice, Obese
Molecular Docking Simulation
Molecular Structure
PPAR alpha
/ agonists
PPAR gamma
/ agonists
Phenylpropionates
/ chemical synthesis
Structure-Activity Relationship
PPAR
SPPARγM
Type 2 diabetes
benzothiazol-2-one
body weight gain
Journal
Journal of enzyme inhibition and medicinal chemistry
ISSN: 1475-6374
Titre abrégé: J Enzyme Inhib Med Chem
Pays: England
ID NLM: 101150203
Informations de publication
Date de publication:
Dec 2020
Dec 2020
Historique:
entrez:
16
1
2020
pubmed:
16
1
2020
medline:
7
3
2020
Statut:
ppublish
Résumé
A series of nitrogen heterocycles containing α-ethoxyphenylpropionic acid derivatives were designed as dual PPARα/γ agonist ligands for the treatment of type 2 diabetes (T2D) and its complications. 6-Benzoyl-benzothiazol-2-one was the most tolerant of the tested heterocycles in which incorporation of O-methyl oxime ether and trifluoroethoxy group followed by enantiomeric resolution led to the (
Identifiants
pubmed: 31939313
doi: 10.1080/14756366.2020.1713771
pmc: PMC7006651
doi:
Substances chimiques
Benzothiazoles
0
Hypoglycemic Agents
0
Ligands
0
PPAR alpha
0
PPAR gamma
0
Phenylpropionates
0
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
524-538Références
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