A p-NITRO ANALOGUE OF PHENYLBUTAZONE POSSESSING POTENT ANTI-RHEUMATIC, SODIUM RETAINING AND URICOSURIC PROPERTIES

¹ The Departments of Medicine, The Mount Sinai Hospital and Columbia University College of Physicians and Surgeons, New York, N. Y.; The Research Service, Third (New York University) Medical Division, Goldwater Memorial Hospital, New York, N. Y.; and the Laboratory of Chemical Pharmacology, National Heart Institute, National Institutes of Health, Bethesda, Maryland
² Departments of Medicine, The Mount Sinai Hospital and Columbia University College of Physicians and Surgeons, New York, N. Y.; The Research Service, Third (New York University) Medical Division, Goldwater Memorial Hospital, New York, N. Y.; and the Laboratory of Chemical Pharmacology, National Heart Institute, National Institutes of Health, Bethesda, Maryland

Studies have been carried out in man with an analogue of phenylbutazone which has a nitro group in the para position of one of the benzene rings. The compound is completely metabolized and disappears with a half-life of about 1 day.

p-Nitrophenylbutazone has pronounced uricosuric properties along with the potent antirheumatic and sodium-retaining effects of phenylbutazone, the first member of the phenylbutazone series to exhibit all three properties in marked degree. The significance of these results in terms of structure-activity relationships in the phenylbutazone series is discussed.