Novel 3-alkyl-2-aryl-3H- naphth [1,2-d]imidazoles were synthesized and evaluated as antiinflammatory agents in the carrageenin-induced paw edema, cotton pellet induced granuloma, and adjuvant-induced polyarthritis assays in rats. The analgesic, antipyretic, and gastroulcerogenic effects were also tested. Structure-activity relationships are discussed. One of the compounds, 3-(1-methylethyl)-2-(4-methoxyphenyl)-3H- naphth [1,2-d]imidazole (35), was selected for clinical trials as a nonacidic antiinflammatory and analgesic agent.

A polyene antibiotic Nystatin injected into the subcutaneous tissues of the rat’s hind-paw provokes a long-lasting localized inflammation. This inflammationis prevented or antagonized by steroidal and non-steroidal anti-inflammatory drugs administered respectively before or after inflammation induction. Among the inhibitors of protein synthesis tested cyclophosphamide, alanosine and 6-mercaptopurine inhibit the development of Nystatin inflammation.

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Die Aminopyrazole (I) werden nach bekannten Methoden zu den Amiden (II) umgesetzt und diese mit POCl3 in siedendem Xylol zu den im Titel genannten Verbindungen (III) cyclisiert.