Potent Thiophene Antagonists of Human Complement C3a Receptor with Anti-Inflammatory Activity.
Animals
Anti-Inflammatory Agents, Non-Steroidal
/ pharmacokinetics
Arginine
/ analogs & derivatives
Benzhydryl Compounds
/ pharmacokinetics
Calcium
/ metabolism
Complement C3a
Hexosaminidases
/ metabolism
Humans
Macrophages
/ drug effects
Mast Cells
Microsomes, Liver
/ drug effects
Rats
Rats, Wistar
Receptors, Complement
/ antagonists & inhibitors
Small Molecule Libraries
Structure-Activity Relationship
Thiophenes
/ chemical synthesis
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 01 2020
23 01 2020
Historique:
pubmed:
8
1
2020
medline:
28
7
2020
entrez:
8
1
2020
Statut:
ppublish
Résumé
Structure-activity relationships for a series of small-molecule thiophenes resulted in potent and selective antagonism of human Complement C3a receptor. The compounds are about 100-fold more potent than the most reported antagonist SB290157. A new compound JR14a was among the most potent of the new antagonists in vitro, assessed by (a) inhibition of intracellular calcium release (IC
Identifiants
pubmed: 31910011
doi: 10.1021/acs.jmedchem.9b00927
doi:
Substances chimiques
Anti-Inflammatory Agents, Non-Steroidal
0
Benzhydryl Compounds
0
Receptors, Complement
0
SB 290157
0
Small Molecule Libraries
0
Thiophenes
0
complement C3a receptor
0
Complement C3a
80295-42-7
Arginine
94ZLA3W45F
Hexosaminidases
EC 3.2.1.-
Calcium
SY7Q814VUP
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM