A large number of oxanilic acid esters and N-heteroaryl oxamic acid esters were prepared and found to have antiallergic activity using the rat passive cutaneous anaphylaxis (PCA) test. Many of the oxanilic acid esters are active orally, with the most active species having an aryl 2'-carbamoyl group and a 3'-methoxy group. Hydrolysis of the ester from the oxanilic ester moiety causes a loss of oral activity.
The uxazole, oxaprozin has a spectrum of activity in various in vivo and in vitro, chronic and acute inflammatory models in 3 species indicating that it belongs to the general class of non-steruidal anti-inflammatory agents. Possible advantageous features of oxaprozin over existing nonsteroidal anti-inflammatory agents include relative safety, minimal irritant properties on the gastrointestinal tract, long half-life, and urieosurie properties.
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