Title :

3-Carboxamido-5-aryl-isoxazoles as new CB2 agonists for the treatment of colitis

Author(s) :

Tourteau, Aurelien [Auteur]
Institut de Chimie Pharmaceutique Albert Lespagnol [ICPAL]
Andrzejak, Virginie [Auteur]
Institut de Chimie Pharmaceutique Albert Lespagnol [ICPAL]
Body-Malapel, Mathilde [Auteur]
Lille Inflammation Research International Center - U 995 [LIRIC]
Lemaire, Lucas [Auteur]
Institut de Chimie Pharmaceutique Albert Lespagnol [ICPAL]
Lemoine, Amelie [Auteur]
Institut de Chimie Pharmaceutique Albert Lespagnol [ICPAL]
Mansouri, Roxane [Auteur]
Institut de Chimie Pharmaceutique Albert Lespagnol [ICPAL]
Djouina, Madjid [Auteur]
Lille Inflammation Research International Center - U 995 [LIRIC]
Renault, Nicolas [Auteur]
Lille Inflammation Research International Center - U 995 [LIRIC]
El Bakali, Jamal [Auteur]

Desreumaux, Pierre [Auteur]
Lille Inflammation Research International Center - U 995 [LIRIC]
Muccioli, Giulio G. [Auteur]
Lambert, Didier M. [Auteur]
Chavatte, Philippe [Auteur]
Lille Inflammation Research International Center - U 995 [LIRIC]
Rigo, Benoit [Auteur]
Leleu, Natascha [Auteur]
Lille Inflammation Research International Center - U 995 [LIRIC]
MILLET, Régis [Auteur]
Lille Inflammation Research International Center - U 995 [LIRIC]

Journal title :

Bioorganic & medicinal chemistry

Abbreviated title :

Bioorg. Med. Chem.

Volume number :

21

Pages :

5383-5394

Publication date :

2013-09-01

ISSN :

0968-0896

English keyword(s) :

CB2
IBD
Isoxazoles
Cannabinoid
Mesh:Mice
Mesh: Animals
Mesh: Anti-Inflammatory Agents/chemistry
Mesh: Anti-Inflammatory Agents/therapeutic use*
Mesh: Anti-Inflammatory Agents/toxicity
Mesh: Cell Proliferation/drug effects
Mesh: Colitis/chemically induced
Mesh: Colitis/drug therapy*
Mesh: Colitis/pathology
Mesh: Dextran Sulfate/toxicity
Mesh: HT29 Cells
Mesh: Humans
Mesh: Interleukin-1beta/genetics
Mesh: Interleukin-1beta/metabolism
Mesh: Isoxazoles/chemistry*
Mesh: Isoxazoles/therapeutic use
Mesh: Isoxazoles/toxicity
Mesh: Male
Mesh: Mice
Mesh: Inbred C57BL
Mesh: Protein Binding
Mesh: Receptor
Mesh: Cannabinoid
Mesh: CB1/agonists
Mesh: Receptor
Mesh: Cannabinoid
Mesh: CB1/metabolism
Mesh: Receptor
Mesh: Cannabinoid
Mesh: CB2/agonists*
Mesh: Receptor
Mesh: Cannabinoid
Mesh: CB2/metabolism
Mesh: Structure-Activity Relationship
Mesh: Tumor Necrosis Factor-alpha/genetics
Mesh: Tumor Necrosis Factor-alpha/metabolism

HAL domain(s) :

Sciences du Vivant [q-bio]

English abstract : [en]

Recent investigations showed that anandamide, the main endogenous ligand of CB1 and CB2 cannabinoid receptors, possesses analgesic, antidepressant and anti-inflammatory effects. In the perspective to treat inflammatory ...
Show more >Recent investigations showed that anandamide, the main endogenous ligand of CB1 and CB2 cannabinoid receptors, possesses analgesic, antidepressant and anti-inflammatory effects. In the perspective to treat inflammatory bowel disease (IBD), our approach was to develop new selective CB2 receptor agonists without psychotropic side effects associated to CB1 receptors. In this purpose, a new series of 3-carboxamido-5-aryl-isoxazoles, never described previously as CB2 receptor agonists, was designed, synthesized and evaluated for their biological activity. The pharmacological results have identified great selective CB2 agonists with in vivo anti-inflammatory activity in a DSS-induced acute colitis mouse model.Show less >

Language :

Anglais

Audience :

Internationale

Popular science :

Non

Administrative institution(s) :

CHU Lille
Inserm
Université de Lille

Collections :

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

Research team(s) :

Therapeutic innovation targetting inflammation

Submission date :

2019-05-17T13:14:32Z
2019-06-05T08:30:46Z
2019-06-06T06:44:51Z
2019-06-06T07:17:52Z
2019-06-06T08:27:41Z
2019-10-07T12:45:20Z