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

Abstract : 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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https://hal.univ-lille.fr/hal-02149143
Contributeur : Lilloa Université de Lille <>
Soumis le : jeudi 6 juin 2019 - 10:41:13
Dernière modification le : mercredi 26 juin 2019 - 01:01:03

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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, Elsevier, 2019, 165, pp.347-362. ⟨10.1016/j.ejmech.2018.12.008⟩. ⟨hal-02149143⟩

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