Titre :

Design, synthesis and evaluation of 2-aryl benzoxazoles as promising hit for the A2A receptor.

Auteur(s) :

Duroux, Romain [Auteur]
Renault, Nicolas [Auteur]
Institut de Recherche Translationnelle sur l'Inflammation (INFINITE) - U1286
Lille Inflammation Research International Center - U 995 [LIRIC]
Cuelho Joana, Esteves [Auteur]
Agouridas, Laurence [Auteur]
Lille Neurosciences & Cognition (LilNCog) - U 1172

Blum, David [Auteur]

Lopes, Luisa [Auteur]
Melnyk, Patricia [Auteur]
Lille Neurosciences & Cognition (LilNCog) - U 1172

Yous, Said [Auteur]
Lille Neurosciences & Cognition (LilNCog) - U 1172

Titre de la revue :

Journal of enzyme inhibition and medicinal chemistry

Nom court de la revue :

J Enzyme Inhib Med Chem

Numéro :

32

Pagination :

850-864

Date de publication :

2017-12-01

ISSN :

1475-6374

Discipline(s) HAL :

Sciences du Vivant [q-bio]

Résumé en anglais : [en]

The development of adenosine A receptor antagonists has received much interest in recent years for the treatment of neurodegenerative diseases. Based on docking studies, a new series of 2-arylbenzoxazoles has been identified ...
Lire la suite >The development of adenosine A receptor antagonists has received much interest in recent years for the treatment of neurodegenerative diseases. Based on docking studies, a new series of 2-arylbenzoxazoles has been identified as potential AR antagonists. Structure-affinity relationship was investigated in position 2, 5 and 6 of the benzoxazole heterocycle leading to compounds with a micromolar affinity towards the A receptor. Compound F1, with an affinity of 1 μm, presented good absorption, distribution, metabolism and excretion properties with an excellent aqueous solubility (184 μm) without being cytotoxic at 100 μm. This compound, along with low-molecular weight compound D1 (K = 10 μm), can be easily modulated and thus considered as relevant starting points for further hit-to-lead optimisation.Lire moins >

Audience :

Internationale

Vulgarisation :

Non

Établissement(s) :

CHU Lille
Inserm
Université de Lille

Collections :

• Institut de Recherche Translationnelle sur l'Inflammation (INFINITE) - U1286
• Lille Neurosciences & Cognition (LilNCog) - U 1172

Équipe(s) de recherche :

Therapeutic innovation targetting inflammation

Date de dépôt :

2019-05-17T13:14:50Z
2021-05-28T09:52:01Z