A new, nonsteroidal antiinflammatory agent, bucloxic acid (CB 804)

Abstract

The 4 (3 chloro 4 cyclohexyl phenyl) 4 oxobutyric acid (bucloxic acid, 804 CB), its methyl ester, its sodium and calcium salts, as well as the 4 (3,5 dichloro 4 cyclohexyl phenyl) 4 oxobutyric acid were prepared. The pharmalogical properties of bucloxic acid were compared with those of its sodium and calcium salts. The first results about the anti inflammatory, analgesic and toxicological activities of these 3 forms of 804 CB, all 3 being administered p.o., showed: the clear superiority of the calcium salt in the experimental granuloma test, the comparable activities of the acid and its calcium salt on the edema phenomena, the better activity of the calcium salt in the carragenin edema test, the better activity of this salt as an analgesic surpassing that of acid form, and the lower toxicity of the calcium salt in mice and to a lesser extent in rats. The calcium form of 804 CB was thus found to be superior. It has been the subject of extensive pharmacological studies, results of which will be reported in detail in further papers.