Synthesis of antiplatelet ortho-carbonyl hydroquinones with differential action on platelet aggregation stimulated by collagen or TRAP-6.
Cell Survival
/ drug effects
Collagen
/ chemistry
Dose-Response Relationship, Drug
Healthy Volunteers
Humans
Hydroquinones
/ chemical synthesis
Molecular Structure
Peptide Fragments
/ chemistry
Platelet Aggregation
/ drug effects
Platelet Aggregation Inhibitors
/ chemical synthesis
Structure-Activity Relationship
Hydroquinone derivatives
Ortho-carbonyl
Platelets
Small molecules
Thrombosis
Journal
European journal of medicinal chemistry
ISSN: 1768-3254
Titre abrégé: Eur J Med Chem
Pays: France
ID NLM: 0420510
Informations de publication
Date de publication:
15 Apr 2020
15 Apr 2020
Historique:
received:
05
12
2019
revised:
23
02
2020
accepted:
24
02
2020
pubmed:
11
3
2020
medline:
1
12
2020
entrez:
11
3
2020
Statut:
ppublish
Résumé
Cardiovascular diseases are the leading cause of death in the world. Platelets have a major role in cardiovascular events as they bind to the damaged endothelium activating and forming thrombi. Although some hydroquinone scaffold-containing compounds have known antiplatelet activities, currently there is a lack of evidence on the antiplatelet activity of hydroquinones carrying electron attractor groups. In this work, we evaluate the antiplatelet effect of a series of ortho-carbonyl hydroquinone derivatives on cytotoxicity and function of human platelets, using collagen and thrombin receptor activator peptide 6 (TRAP-6) as agonists. Our structure-activity relationship study shows that gem-diethyl/methyl substitutions and the addition/modifications of the third ring of ortho-carbonyl hydroquinone scaffold influence on the selective index (IC
Identifiants
pubmed: 32155530
pii: S0223-5234(20)30154-9
doi: 10.1016/j.ejmech.2020.112187
pii:
doi:
Substances chimiques
Hydroquinones
0
Peptide Fragments
0
Platelet Aggregation Inhibitors
0
thrombin receptor peptide (42-47)
0
Collagen
9007-34-5
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
112187Informations de copyright
Copyright © 2020 Elsevier Masson SAS. All rights reserved.
Déclaration de conflit d'intérêts
Declaration of competing interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.