Synthesis and Biological Evaluation of New Antiinflammatory 1-Benzothiophene-2-carboxanilides

3-Substituted 1-benzothiophene-2-carboxanilides 2-5 and their corresponding sulfones 6-8 were synthesized. The antiinflammatory effect of compounds 2-8 was evaluated in tests of LTB4 biosynthesis, carrageenin edema and ear inflammation. With the exception of 3-hydroxyamides 5a-5c, low inhibitory activities against COX and LT biosynthesis were observed.

Reaction of 4-aroyl-2(3H)-dihydrofuranones with hydroxylamine hydrochloride. Synthesis and pharmacological study of a series of 3-aryl-4,5-dihydro-4-isoxazoleacetic acids

We have synthesized and tested for their antiinflammatory activity a new series of 3-aryl-4,5-dihydro-4-isoxazoleacetic acids (IVa-IVg). Preliminary pharmacological results seem to indicate the 3-phenyl derivative IVa as the most interesting compound. In fact, when tested against carrageenin edema in Wistar rats, it shows antiinflammatory activity comparable to that of naproxene, taken as reference drug, though of shorter duration. All the substituted phenyl derivatives were less active (IVd-IVf) or inactive (IVb, IVc, IVg).