Amide derivatives of [6-acyl-2-benzothiazolinon-3-yl] acetic acids as potential analgesic and anti-inflammatory compounds

作者：Onkol Tijen^*; Banoglu Erden; Dundar Yasemin; Kupeli Esra; Sahin M Fethi

来源：Medicinal Chemistry Research, 2010, 19(1): 11-24.

DOI：10.1007/s00044-009-9168-x

• Benzothiazolinone
• Analgesic
• Anti-inflammatory
• 5-LOX
• COX-1
• COX-2

In this study, we investigated the analgesic and anti-inflammatory activities of [6-acyl-2-benzothiazolinon-3-yl]acetic acids by the derivatization of the carboxylate moiety into amides. We have tested the analgesic and anti-inflammatory activities of the synthesized compounds in vivo by using p-benzoquinone-induced writhing test and carrageenan-induced hind paw edema model, respectively. Compounds 4h, 4i, 4n, and 4o showed comparable analgesic and anti-inflammatory activities to the references without gastric lesions in the tested animals. In addition, all compounds also tested for their inhibitory activity against cyclooxygenase (COX)-1, COX-2 and 5-lipoxygenase (LOX), but no significant inhibition was observed under assayed conditions.

• 出版日期2010-2