Yous S, Poupaert J H, Chavatte P, Espiard J G, Caignard D H, Lesieur D
Laboratoire de Chimie Thérapeutique, Faculté des Sciences Pharmaceutiques et Biologiques, Lille, France.
Drug Des Discov. 2001;17(4):331-6.
A series of novel 6-substituted-2(3H)-benzothiazolones were synthesized and studied as analgesic agents. Among these compounds, two of them were found to exhibit potent analgesic activity in several in vivo tests (acetic acid writhing, Koster, carrageenan and PGE2 hyperalgesia). In these tests the most active compound of this series, i.e. 6-benzoyl-2(3H)-benzothiazolone (4a) was found to be superior to acetylsalicylic acid and equivalent to glafenine. The present study allows to conclude that 4a represents a new type of antinociceptive agent acting in periphery by inhibiting the cyclo-oxygenase pathway and promoting the release of an opioid peptide.
合成了一系列新型的6-取代-2(3H)-苯并噻唑酮并作为镇痛药进行了研究。在这些化合物中，发现其中两种在多项体内试验（乙酸扭体、科斯特试验、角叉菜胶试验和前列腺素E2致痛试验）中表现出强效镇痛活性。在这些试验中，该系列中最具活性的化合物，即6-苯甲酰基-2(3H)-苯并噻唑酮（4a）被发现优于乙酰水杨酸且等同于格拉非宁。本研究可以得出结论，4a代表了一种新型的抗伤害感受剂，它通过抑制环氧化酶途径并促进阿片肽的释放而在外周发挥作用。
