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R-830, a di-tert-butylphenol, has been shown to be anti-inflammatory in a number of animal models. These include conventional systems such as carrageenan-induced edema and adjuvant arthritis of the rat and ultraviolet-induced erythema in the guinea pig in which the acidic nonsteroidal anti-inflammatory drugs (e.g., indomethacin) are effective. The anti-inflammatory activity of R-830 has also been demonstrated in other models (e.g., graft vs. host reaction and reversed passive cutaneous Arthus reaction in the rat, contact sensitivity in the mouse) in which the acidic nonsteroidal drugs are not effective. In vitro, R-830 inhibits guinea pig lung lipoxygenase and bovine seminal vesicle cyclo-oxygenase. The antioxidant properties of R-830 were demonstrated in two in vitro systems. We speculate that the antioxidant activity of this molecule might be related to its unusual profile of pharmacological activity.

A series of isosteres of 3-benzoyltrifluoromethanesulfonanilide involving alternatives to the carbonyl linking group was synthesized and screened for antiinflammatory activity in the carrageenan rat paw edema test. The systems examined were of the type m-CF3SO2NH-C6H4-X-C6H5, where X was -CROH-, -CHR-, -CH(OH)CH2-, -COCH2-, -CH2CO-, greater than C equal to CR2, -CR equal to CH, -C identical to C-, -CH2CH2-, CONH-, -NR-, -O-, -S(O)n- (n equal to 0,1,2), and carbon-carbon single bond. Many ortho and para derivatives were also tested. Several of these new trifluoromethanesulfonanilides proved equipotent with phenylbutazone. The effects on the anticarrageenan activity of both the nature and ring position of X are discussed.

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