Discovery of Novel Pterostilbene-Based Derivatives as Potent and Orally Active NLRP3 Inflammasome Inhibitors with Inflammatory Activity for Colitis.
Animals
Anti-Inflammatory Agents
/ chemical synthesis
Cell Line
Colitis
/ chemically induced
Dextran Sulfate
Female
Humans
Inflammasomes
/ antagonists & inhibitors
Interleukin-1beta
/ antagonists & inhibitors
Macrophages
/ drug effects
Male
Mice, Inbred C57BL
Molecular Structure
NLR Family, Pyrin Domain-Containing 3 Protein
/ antagonists & inhibitors
Pyroptosis
/ drug effects
Stilbenes
/ chemical synthesis
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:
23 09 2021
23 09 2021
Historique:
pubmed:
11
9
2021
medline:
15
12
2021
entrez:
10
9
2021
Statut:
ppublish
Résumé
Studies have shown that the abnormal activation of the NLRP3 inflammasome is involved in a variety of inflammatory-based diseases. In this study, a high content screening model targeting the activation of inflammasome was first established and pterostilbene was discovered as the active scaffold. Based on this finding, total of 50 pterostilbene derivatives were then designed and synthesized. Among them, compound
Identifiants
pubmed: 34506712
doi: 10.1021/acs.jmedchem.1c01007
doi:
Substances chimiques
Anti-Inflammatory Agents
0
IL1B protein, mouse
0
Inflammasomes
0
Interleukin-1beta
0
NLR Family, Pyrin Domain-Containing 3 Protein
0
Nlrp3 protein, mouse
0
Stilbenes
0
pterostilbene
26R60S6A5I
Dextran Sulfate
9042-14-2
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM