Article (Scientific journals)
Synthesis of ticagrelor analogues belonging to 1,2,3-triazolo[4,5-d]pyrimidines and study of their antiplatelet and antibacterial activity.
Goffin, Eric; Jacques, Nicolas; Musumeci, Lucia et al.
2020In European Journal of Medicinal Chemistry, 208, p. 112767
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Synthesis of ticagrelor analogues belonging to 123-triazolo45-d pyrimidines and study of their antiplatelet and antibacterial activity.pdf
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Keywords :
1,2,3-triazolo[4,5-d]pyrimidines; 8-Azapurines; Antibiotics; Antiplatelet agents; Ticagrelor
Abstract :
[en] Based on the recent observation that the antiplatelet agent ticagrelor and one of its metabolite exert bactericidal activity against gram-positive bacteria, a series of 1,2,3-triazolo[4,5-d]pyrimidines structurally related to ticagrelor were synthesized and examined as putative antiplatelet and antibacterial agents. The aim was to assess the possibility of dissociating the two biological properties and to find novel 1,2,3-triazolo[4,5-d]pyrimidines expressing antiplatelet activity and devoid of in vitro antibacterial activity. The new compounds synthesized were known metabolites of ticagrelor as well as structurally simplified analogues. Some of them were found to express antiplatelet activity and to lose the antibacterial activity, supporting the view that the two activities were not necessarily linked.
Disciplines :
Cardiovascular & respiratory systems
Author, co-author :
Goffin, Eric ;  Université de Liège - ULiège > Cardiovascular Sciences-Cardiology
Jacques, Nicolas 
Musumeci, Lucia ;  Université de Liège - ULiège > Cardiovascular Sciences-Cardiology
Nchimi Longang, Alain 
Oury, Cécile  ;  Université de Liège - ULiège > Cardiovascular Sciences-Cardiology
Lancellotti, Patrizio  ;  Université de Liège - ULiège > Département des sciences cliniques > Cardiologie - Pathologie spéciale et réhabilitation
Pirotte, Bernard ;  Université de Liège - ULiège > Département de pharmacie > Chimie pharmaceutique
Language :
English
Title :
Synthesis of ticagrelor analogues belonging to 1,2,3-triazolo[4,5-d]pyrimidines and study of their antiplatelet and antibacterial activity.
Publication date :
2020
Journal title :
European Journal of Medicinal Chemistry
ISSN :
0223-5234
eISSN :
1768-3254
Publisher :
Elsevier, Netherlands
Volume :
208
Pages :
112767
Peer reviewed :
Peer Reviewed verified by ORBi
Commentary :
Copyright © 2020 Elsevier Masson SAS. All rights reserved.
Available on ORBi :
since 23 October 2020

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