REVIEW Sulfametoxydiazine or sulfamethoxydiazine (sulfameter) is a long-acting sulfonamide antibacterial, encompassing most gram-positive and many gram-negative organisms. It is used as a leprostatic agent and in the treatment of urinary tract infections. Sulfameter and all sulfonamide anitbacterials are antimetabolites, whereby the sulfonamidecompete with para-aminobenzoic acid (PABA) for incorporation into folic acid. The action of sulfonamides illustrates the principle of selective toxicity where some difference between mammal cells and bacterial cells is exploited. All cells require folic acid for growth. Folic acid (as a vitamin is in food) diffuses or is transported into human cells. However, folic acid cannot cross bacterial cell walls by diffusion or active transport. For this reason bacteria must synthesize folic acid from p-aminobenzoic acid.
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Bass, Allan D.; Weinstein, Ira Chemotherapy of bacterial infections. II. Sulfonamides , Edited by DiPalma, Joseph R , Drill's Pharmacol. Med., 4th Ed. (1971), 1657-73.
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Sammes, Peter G. Sulfonamides and sulfones Edited by Hansch, Corwin; Sammes, Peter G.; Taylor, John B, Comprehensive Medicinal Chemistry (1990), 2, 255-270.
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Budesinsky, Z.; Bydzovsky, V.; Prikryl, J.; Svab, J. Sulfonamides with protracted antibacterial activity. I. 2-Sulfanilamidoalkoxypyrimidines Cesko-Slovenska Farmacie (1961), 10, 14-20.
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Horstmann, H.; Knott, Th.; Scholtan, W.; Schraufstaetter, E.; Walter, A.; Woerffel, U Relations between structure activity and protein binding in the 2-sulfanilamidopyrimidine series Arzneimittel-Forschung (1961), 11, 682-4.
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