非甾体抗炎药4-(2-噻吩羰基)苯酚类化合物的抗炎活性

Anti-inflammatory Activity of New Non-steroidal Antiinflammatory Agent: Derivatives of 4-(2-Thiophene Carbonyl)-Phenol Compounds

非甾体类抗炎药临床上用于治疗风湿性关节炎及其它胶原性疾病。国内外正不断地寻找新的化合物。我们曾发现氨甲基酚类化合物有较好的抗炎活性。

Five derivatives of 4-(2-thiophene-carbonyl)-phenol compounds were tested for their anti-inflammatory activity, with substituents of -N-methylene-pyridine, -N-methylene-N'-methyl-piperazine, and -N-methylene-N'-p-fluoro-phenyl-piperazine on the 2 and 6 position of benzene ring. It was shown that significantly inhibitory effect was evidenced on the swellings induced by either the Freund's complete adjuvant or carrageenin. The compounds were characterised as a class of non-steroidal anti-inflammatory agents of the short duration and moderate potency, possibly being as potent as indomethacin. Among the compounds the most acutely toxic was TH_2, but, TH_4 and TH_5 were more effective and less toxic.