Recently, Robin and his associates1 have described the preparation of certain heterocyclic sulfonamide compounds. Among them were 2-sulfanilamido-pyrimidine, 2 N4-acetylsulfanilamidopyrimidine, 2-sulfanilamido-4-methylpyrimidine, 2-N4-acetylsulfanilamido-4-methylpyrimidine and 4-sulfanilamidopyrimidine. One of these compounds, 2-sulfanilamidopyrimidine, to which the name of sulfadiazine has been given in order to prevent confusing this pyrimidine derivative with the pyridine homologue of sulfanilamide, has been distributed for experimental use and clinical investigation. The name sulfadiazine has been accepted by the Council on Pharmacy and Chemistry.
Feinstone and his collaborators2 have made an excellent and complete report on the toxicity, absorption and chemotherapeutic activity of this compound in experimental animals. As regards the acute toxicity of sulfadiazine for mice, based on blood concentrations, they found that the L. D. 50 (i. e., the blood concentration of the drug which kills 50 per cent of the mice) lay between 175 and 200 mg. per hundred cubic centimeters.
LONG PH. SULFADIAZINE: THE 2-SULFANILAMIDOPYRIMIDINE ANALOGUE OF SULFANILAMIDE. JAMA. 1941;116(21):2399–2401. doi:10.1001/jama.1941.62820210007009
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