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

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 (Ki = 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.

journal_name

Eur J Med Chem

authors

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

doi

10.1016/j.ejmech.2018.12.008

subject

Has Abstract

pub_date

2019-03-01 00:00:00

pages

347-362

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(18)31045-6

journal_volume

165

pub_type

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