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 Chemjournal_title
European journal of medicinal chemistryauthors
Leleu-Chavain N,Baudelet D,Heloire VM,Rocha DE,Renault N,Barczyk A,Djouina M,Body-Malapel M,Carato P,Millet Rdoi
10.1016/j.ejmech.2018.12.008subject
Has Abstractpub_date
2019-03-01 00:00:00pages
347-362eissn
0223-5234issn
1768-3254pii
S0223-5234(18)31045-6journal_volume
165pub_type
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