Switching cannabinoid response from CB2 agonists to FAAH inhibitors | Tourteau, Aurélien
/5

0 avis

Switching cannabinoid response from CB2 agonists to FAAH inhibitors

Archive ouverte : Article de revue

Tourteau, Aurélien | Leleu-Chavain, Natascha | Body-Malapel, Mathilde | Andrzejak, Virginie | Barczyk, Amelie | Djouina, Madjid | Rigo, Benoit | Desreumaux, Pierre | Chavatte, Philippe | Millet, Régis

Edité par HAL CCSD ; Elsevier

International audience. A series of 3-carboxamido-5-aryl-isoxazoles designed as CB2 agonists were evaluated as FAAH inhibitors. The pharmacological results led to identify structure-activity relationships enabling to switch cannabinoid response from CB2 agonists to FAAH inhibitors. Two compounds were selected for their FAAH and/or CB2 activity, and evaluated in a colitis model for their anti-inflammatory activity. Results showed that compounds 10 and 11 inhibit the development of DSS-induced acute colitis in mice and then, are interesting leads to explore new drug candidates for IBD.

Consulter en ligne

Suggestions

Du même auteur

Pyroglutamide-Based P2X7 Receptor Antagonists Targeting Inflammatory Bowel Disease | Homerin, Germain

Pyroglutamide-Based P2X7 Receptor Antagonists Targeting Inflammatory Bowel ...

Archive ouverte: Article de revue

Homerin, Germain | 2019-09-27

International audience. This report deals with the design, the synthesis, and the pharmacological evaluation of pyroglutamide-based P2X7 antagonists. A dozen were shown to possess improved properties, among which in...

A small-molecule P2RX7 activator promotes anti-tumor immune responses and sensitizes lung tumor to immunotherapy | Douguet, Laetitia

A small-molecule P2RX7 activator promotes anti-tumor immune responses and s...

Archive ouverte: Article de revue

Douguet, Laetitia | 2021-12

International audience. Only a subpopulation of non-small cell lung cancer (NSCLC) patients responds to immunotherapies, highlighting the urgent need to develop therapeutic strategies to improve patient outcome. We ...

Phenyliodine(III) Diacetate/I 2 ‐Mediated Domino Approach for Pyrrolo[1,4]Thiazines and 1,4‐Thiazines by a One‐Pot Morin Rearrangement of N,S ‐ Acetals | Danton, Fanny

Phenyliodine(III) Diacetate/I 2 ‐Mediated Domino Approach for Pyrrolo[1,4]T...

Archive ouverte: Article de revue

Danton, Fanny | 2019-02-22

International audience. An efficient domino transformation using a phenyliodine(III) diacetate (PIDA)/I2 combination towards Morin 1,4-thiazine compounds has been developed starting from N,S-acetals. The latter lead...

Du même sujet

Lactose derivatives as potential inhibitors of pectin methylesterases | L’enfant, Mélanie

Lactose derivatives as potential inhibitors of pectin methylesterases

Archive ouverte: Article de revue

L’enfant, Mélanie | 2019-07

International audience. The discovery of molecules that can inhibit the action of phytopathogens is essential to find alternative to current pesticides. Pectin methylesterases (PME), enzymes that fine-tune the degre...

Tuning the Selectivity: Study of Solvent-Free Acid-Mediated Pinacolic-Pinacolone Rearrangement under Microwave Irradiation | Billamboz, Muriel

Tuning the Selectivity: Study of Solvent-Free Acid-Mediated Pinacolic-Pinac...

Archive ouverte: Article de revue

Billamboz, Muriel | 2018-09-28

International audience

Antimicrobial and antioxidant activities of amines derived from vanillin as potential preservatives: Impact of the substituent chain length and polarity | Fayeulle, Antoine

Antimicrobial and antioxidant activities of amines derived from vanillin as...

Archive ouverte: Article de revue

Fayeulle, Antoine | 2021-09

International audience

Repeated photoporation with graphene quantum dots enables homogeneous labeling of live cells with extrinsic markers for fluorescence microscopy | Liu, Jing

Repeated photoporation with graphene quantum dots enables homogeneous label...

Archive ouverte: Article de revue

Liu, Jing | 2018-08-08

International audience. In the replacement of genetic probes, there is increasing interest in labeling living cells with high-quality extrinsic labels, which avoid over-expression artifacts and are available in a wi...

Microplastic leachates disrupt the chemotactic and chemokinetic behaviours of an ecosystem engineer (Mytilus edulis) | Uguen, Marine

Microplastic leachates disrupt the chemotactic and chemokinetic behaviours ...

Archive ouverte: Article de revue

Uguen, Marine | 2022

International audience. The massive contamination of the environment by plastics is an increasing global scientific and societal concern. Knowing whether and how these pollutants affect the behaviour of keystone spe...

Proteolytic activity of Lactobacillus strains isolated from Mongolian traditional dairy products: A multiparametric analysis | Raveschot, Cyril

Proteolytic activity of Lactobacillus strains isolated from Mongolian tradi...

Archive ouverte: Article de revue

Raveschot, Cyril | 2020-01-30

Chargement des enrichissements...