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.

CB ₂受体在免疫细胞中的高度分布表明它们在炎症控制中的重要作用。越来越多的证据提供这种受体作为有吸引力的治疗靶标：选择性的CB ₂激动剂能够调节炎症而不触发精神作用。在这项工作中，我们报告了一系列基于苯并[ d ]噻唑-2（3H）-一个支架的选择性CB ₂激动剂的新系列。该药物设计项目促成化合物9的发现，它是一种非常有效的CB ₂激动剂（K _i  = 13.5 nM），相对于CB ₁具有良好的选择性。该化合物未显示细胞毒性，可接受的ADME-Tox参数，并显示出在体内抵抗结肠炎性过程的能力。