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

Basic Information

ID: ALA4480384

Journal: Eur J Med Chem

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

Authors: Leleu-Chavain N, Baudelet D, Heloire VM, Rocha DE, Renault N, Barczyk A, Djouina M, Body-Malapel M, Carato P, Millet R.

Abstract: The high distribution of CB₂ receptors in immune cells suggests their important role in the control of inflammation. Growing evidence offers this receptor as an attractive therapeutic target: selective CB₂ agonists are able to modulate inflammation without triggering psychotropic effects. In this work, we report a new series of selective CB₂ 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 CB₂ agonist (K_i = 13.5 nM) with a good selectivity versus CB₁. This compound showed no cytotoxicity, acceptable ADME-Tox parameters and demonstrates the ability to counteract colon inflammatory process in vivo.

CiteXplore: 30583970

DOI: 10.1016/j.ejmech.2018.12.008

Patent ID: ┄

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