Methanesulfonyl Amino Group, The Synthesis Of Ammonia Sulfonyl Thiophene Compounds And Anti-inflammatory Analgesic Role

The synthesis and anti-inflammatory, analgesic activities of methanesulfonylamino and aminosulfonyl thiophenes were reported in this paper.Research for dual COX/5-LOX inhibitors has been an important field currently for new anti-inflammatory and analgesic agents with high efficacy and minimal side-effects. It was reported that RWJ-63556, one of 5-phenoxyl-2-methanesulfonylaminothiophenes, showed dual COX-2/5-LOX inhibition in vitro. Based on the structure of RWJ-63556, nine analogs were designed and synthesized.Pharmacological studies showed that, with the dose of 200mg/kg, most of the compounds have potent anti-inflammatory and analgesic activities on mice. The results provided basis for further study on SAR and development of new NSAIDs.