Benzo[d]thiazol-2(3H)-ones as new potent selective CB2 agonists with anti-inflammatory properties. - Université de Lille Accéder directement au contenu
Article Dans Une Revue European Journal of Medicinal Chemistry Année : 2019

Benzo[d]thiazol-2(3H)-ones as new potent selective CB2 agonists with anti-inflammatory properties.

Résumé

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.
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hal-02149143 , version 1 (21-10-2021)

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Natascha Leleu-Chavain, Davy Baudelet, Valéria Moas Heloire, Diana Escalante Rocha, Nicolas Renault, et al.. Benzo[d]thiazol-2(3H)-ones as new potent selective CB2 agonists with anti-inflammatory properties.. European Journal of Medicinal Chemistry, 2019, 165, pp.347-362. ⟨10.1016/j.ejmech.2018.12.008⟩. ⟨hal-02149143⟩
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