Studies on the synthesis and anti-inflammatory activity of 2,6-di-tert-butylphenols with a heterocyclic group at the 4-position. I.

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Abstract
A number of 2,6-di-tert-butylphenols with a heterocyclic group at the 4-position were prepared. The heterocyclic groups were as follows: benzoxazole, benzothiazole, benzimidazole, indole, imidazo[1,2-a]pyridine and imidazo[1,2-a]pyrimidine. Antiinflammatory activity of these compounds was examined by using the adjuvant-induced arthritis (A.A) assay. Some compounds were further tested in carrageenan-induced rat paw edema (CIPE) assay and AcOH[acetyl hydroxide]-induced writhing (AIW) assay in mice. The antiinflammatory activity was greatly dependent on the value of the heterocyclic group. Among these compounds, 2-(3,5-di-tert-butyl-4-hydroxyphenyl)-benzoxazole and 2-(3,5-di-tert-butyl-4-hydroxyphenyl)indole showed very potent activity. Both had a minimum effective dose of 5 mg/kg (p.o.[orally]) in A.A. assay and showed stronger activity than phenylbutazone in CIPE assay, but weaker analgesic activity than aminopyrine in AIW assay.

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