Title :

Benzo[d]thiazol-2(3H)-ones as new potent selective CB agonists with anti-inflammatory properties.

Author(s) :

Leleu-Chavain, Natascha [Auteur]
Institut de Chimie Pharmaceutique Albert Lespagnol [ICPAL]
Baudelet, Davy [Auteur]
Institut de Chimie Pharmaceutique Albert Lespagnol [ICPAL]
Heloire, Valéria Moas [Auteur]
Rocha, Diana Escalante [Auteur]
Renault, Nicolas [Auteur]
Lille Inflammation Research International Center - U 995 [LIRIC]
Barczyk, Amélie [Auteur]
Djouina, Madjid [Auteur]
Lille Inflammation Research International Center - U 995 [LIRIC]
Body-Malapel, Mathilde [Auteur]
Lille Inflammation Research International Center - U 995 [LIRIC]
Carato, Pascal [Auteur]
MILLET, Régis [Auteur]
Lille Inflammation Research International Center - U 995 [LIRIC]

Journal title :

European journal of medicinal chemistry

Abbreviated title :

Eur J Med Chem

Volume number :

165

Pages :

347-362

Publication date :

2019-03-01

ISSN :

1768-3254

English keyword(s) :

Anti-Inflammatory Agents
Benzothiazoles
Cannabinoid Receptor Agonists
Colon
Humans
Inflammation
Receptor
Cannabinoid
CB2
Structure-Activity Relationship
CB(2) agonist
Colon inflammatory
Inflammation

HAL domain(s) :

Sciences du Vivant [q-bio]

English abstract : [en]

The high distribution of CB receptors in immune cells suggests their important role in the control of inflammation. Growing evidence offers this receptor as an attractive therapeutic target: selective CB agonists are able ...
Show more >The high distribution of CB receptors in immune cells suggests their important role in the control of inflammation. Growing evidence offers this receptor as an attractive therapeutic target: selective CB agonists are able to modulate inflammation without triggering psychotropic effects. In this work, we report a new series of selective CB agonists based on a benzo[d]thiazol-2(3H)-one scaffold. This drug design project led to the discovery of compound 9, as a very potent CB agonist (K = 13.5 nM) with a good selectivity versus CB. This compound showed no cytotoxicity, acceptable ADME-Tox parameters and demonstrates the ability to counteract colon inflammatory process in vivo.Show less >

Language :

Anglais

Audience :

Non spécifiée

Collections :

• Institut de Recherche Translationnelle sur l'Inflammation (INFINITE) - U1286

Research team(s) :

Therapeutic innovation targetting inflammation
IBD and environnemental factors : epidemiology and functional analyses

Submission date :

2019-05-20T15:10:29Z
2019-06-06T08:39:26Z
2019-06-06T08:41:05Z