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British Journal of Pharmacology and ChemotherapyVolume 33, Issue 1 p. 72-90 Free Access TRIMETHOPRIM, A SULPHONAMIDE POTENTIATOR S. R. M. BUSHBY, S. R. M. BUSHBY Wellcome Research Laboratories, Beckenham, Kent, and Tuckahoe, New YorkSearch for more papers by this authorG. H. HITCHINGS, G. H. HITCHINGS Wellcome Research Laboratories, Beckenham, Kent, and Tuckahoe, New YorkSearch for more papers by this author S. R. M. BUSHBY, S. R. M. BUSHBY Wellcome Research Laboratories, Beckenham, Kent, and Tuckahoe, New YorkSearch for more papers by this authorG. H. HITCHINGS, G. H. HITCHINGS Wellcome Research Laboratories, Beckenham, Kent, and Tuckahoe, New YorkSearch for more papers by this author First published: May 1968 https://doi.org/10.1111/j.1476-5381.1968.tb00475.xCitations: 288AboutPDF ToolsRequest permissionExport citationAdd to favoritesTrack citation ShareShare Give accessShare full text accessShare full-text accessPlease review our Terms and Conditions of Use and check box below to share full-text version of article.I have read and accept the Wiley Online Library Terms and Conditions of UseShareable LinkUse the link below to share a full-text version of this article with your friends and colleagues. Learn more.Copy URL Share a linkShare onFacebookTwitterLinkedInRedditWechat References Anton, A. H. (1960). The relation between the binding of sulfonamides to albumin and their antibacterial efficacy. J. Pharmac. exp. Ther., 129, 282– 290. Bratton, A. C., Marshall, E. K. Jr., Babbit, D. & Hendrickson, A. R. (1939). A new coupling component for sulfanilamide determination. J. biol. Chem., 128, 537– 550. Burchall, J. J. & Hitchings, G. H. (1965). Inhibitor binding analysis of dihydrofolate-reductases from various species. Molec. Pharmac., 1, 126– 136. Bushby, S. R. M. & Barnett, M. (1967). Trimethoprim-sulphonamides. In vitro sensitivity of 384 strains of bacteria. Proceedings 5th International Congress of Chemotherapy Vienna, 753– 757. Clarke, M. L. (1962). A mixture of diaveridine and sulphaquinoxaline as a coccidiostat for poultry. I. Preliminary studies on efficiency against Eimeria tenella and E. necatrix infections, and on toxicity in poultry. Vet. Rec., 74, 845– 848. Cooper, R. G. & Wald, M. (1964). Successful treatment of proteus septicaemia with a new drug, trimethoprim. Med. J. Aust, 93– 96. Czonka, G. J. (1967). Therapeutic trial of trimethoprim as a potentiator of sulphonamides in gonorrhoea. Br. J. vener. Dis., 43, 161– 165. Drew, C. D. M., Hughes, D. T. D. & Jenkins, G. C. (1967). Long-term treatment of chest infections with a combination of trimethoprim and a sulphonamide. A study of the clinical bacteriological and haematological effects. Proceedings 5th International Congress of Chemotherapy Vienna June Supplement, p. 107. Drew, C. D. M., Hughes, D. T. D., Fowle, A. S. E. & Cassell, M. A. (1967). Effective treatment of chronic bronchitis with short-term trimethoprim and sulphamethoxazole. Proceedings 5th International Congress of Chemotherapy Vienna June 2, 293– 296. Elion, G. B., Singer, S. & Hitchings, G. H. (1954). Antagonists of nucleic acid derivatives. VIII. Synergism in combinations of biochemically related antimetabolites. J. biol. Chem., 208, 477– 488. Eyles, D. E. & Coleman, N. (1953). Synergistic effect of sulfadiazine and Daraprim against experimental toxoplasmosis in the mouse. Antibiotics Chemother., 3, 483– 490. Falco, E. A., Hitchings, G. H., Russell, P. B. & Vanderwerff, H. (1949). Antimalarials as antagonists of purines and pteroylglutamic acid. Nature Lond., 164, 107– 108. Frenkel, J. K. & Hitchings, G. H. (1957). Relative reversal by vitamins (p-aminobenzoic, folic, and folinic acids) of the effects of sulfadiazine and pyrimethamine on toxoplasma, mouse and man. Antibiotics Chemother., 7, 630– 638. Garrod, L. P. & Waterworth, P. M. (1967). The Antibacterial action of trimethoprim. Proceedings 5th International Congress of Chemotherapy Vienna June 2, 747– 751. Hitchings, G. H. (1960). Pyrimethamine. The use of an antimetabolite in the chemotherapy of malaria and other infections. Clin. Pharmac. Ther., 1, 570– 589. Hitchings, G. H. (1961). A biochemical approach to chemotherapy. Trans N.Y. Acad. Sci., 23, 700– 708. Hitchings, G. H. (1962). The utilisation of biochemical differences between host and parasite as a basis for chemotherapy. Biological Council Symposium on Drugs, Parasites and Hosts, ed. L. G. Goodwin & Smith. R. H. Nimmo, pp. 196– 210. Hitchings, G. H. (1964). Antimetabolites and chemotherapy: Integration of biochemistry and molecular manipulation. Chemotherapy of Cancer, ed. P. A. Plattner, pp. 77– 87. Amsterdam: Elsevier Publishing Co. Hitchings, G. H. & Burchall, J. J. (1965). Inhibition of folate biosynthesis and function as a basis for chemotherapy. Advances in Enzymology, ed. F. F. Nord, vol. 27, pp. 417– 468. New York: John Wiley & Sons, Inc. Interscience Publishers Div. Hitchings, G. H., Burchall, J. J. & Ferone, R. (1966a). The comparative enzymology of dihydrofolate reductase and the design of chemotherapeutic agents. Symposia of the Society for General Microbiology. Biochemical Studies of Antimicrobial Drugs, pp. 294– 300. Hitchings, G. H., Burchall, J. J. & Ferone, R. (1966b). Comparative enzymology of dihydrofolate reductases as a basis for chemotherapy. Proceedings IIIrd International Pharmacological Congress, Sao Paulo, Brazil. Abstracts 113. Hitchings, G. H. & Bushby, S. R. M. (1961). 5-Benzyl-2,4-diaminopyrimidines, a new class of systemic antibacterial agents. 5th Int. Congress Biochem. Moscow, p. 165. Hitchings, G. H., Elion, G. B., Falco, E. A., Russell, P. B., Sherwood, M. B. & Vanderwerff, H. (1950). Antagonists of nucleic acid derivatives. I. The Lactobacillus casei model. J. biol. Chem., 183, 1– 9. Hitchings, G. H., Elion, G. B., Falco, E. A., Russell, P. B. & Vanderwerff, H. (1950). Studies on analogs of purines and pyrimidines. Ann. N.Y. Acad. Sci., 52, 1318– 1335. Hitchings, G. H., Elion, G. B. & Singer, S. (1954). Chemistry and biology of pteridines, ed. Wolstenholme, pp. 290– 303. London: Churchill. Hitchings, G. H., Elion, G. B., Vanderwerff, H. & Falco, E. A. (1948). Pyrimidine derivatives as antagonists of pteroylglutamic acid. J. biol. Chem., 174, 765– 766. Hitchings, G. H., Falco, E. A., Elion, G. B., Singer, S., Waring, G. B., Hutchison, D. J. & Burchenall, J. H. (1952). 2,4-Diamino-pyrimidines as antagonists of folic acid and folinic acid. Archs Biochem. Biophys., 40, 479– 481. Hitchings, G. H., Falco, E. A. & Ledig, K. W. (1958). To Burroughs Wellcome & Co. U.S. Patent 2,945,859, Dec. 15, 1958. Hitchings, G. H., Falco, E. A., Vanderwerff, H., Russell, P. B. & Elion, G. B. (1952). Antagonists of nucleic acid derivatives. VII. 2,4-Diaminopyrimidines. J. biol. Chem., 199, 43– 56. Hitchings, G. H., Herrmann, T. A., Hurlbert, B. S. & Bushby, S. R. M. (1964). 2,4-Diaminopyrido-(2,3-d)pyrimidines: A new group of antibacterial agents. Proceedings 3rd International Congress of Chemotherapy, Stuttgart, p. 1363. Jukes, T. H. & Broquist, H. P. (1963). Sulphonamides and folic acid antagonists. Metabolic Inhibitors, ed. R. M. Hochester & J. H. Quastel, 1st ed., p. 481. New York: Academic Press. Kahn, S. B. & Brodsky, I. (1967). Effects of trimethoprim (TMP) on folate metabolism in man. Clin. Res., XV, 281. Lux, R. E. (1954). The chemotherapy of Eimeria tenella. I. Diaminopyrimidines and dihydrotriazines. Antibiotics Chemother., 4, 971– 977. Noall, E. W. P., Sewards, H. F. G. & Waterworth, P. M. (1962). Successful treatment of a case of proteus septicaemia. Br. med. J., 2, 1101– 1102. O'Meara, R. A. Q. (1931). A simple delicate and rapid method of detecting the formation of acetylmethyl carbinol by bacteria fermenting carbohydrate. J. Path., 34, 401– 406. Peizer, L. R. & Schecter, E. (1950). A new medium for bacteriologic diagnosis of tuberculosis. Am. J. clin. Path., 20, 682– 685. Robins, R. K. & Hitchings, G. H. (1955). Studies on condensed pyrimidine systems. XII. Synthesis of some 4- and 2,4-substituted pyrido(2,3-d)pyrimidines. J. Am. Chem. Soc., 77, 2256– 2260. Robins, R. K. & Hitchings, G. H. (1958). Studies on condensed pyrimidine systems. XIX. A new synthesis of pyrido(2,3-d)pyrimidines. The condensation of 1,3-diketones and 3-ketoaldehydes with 4-amino-pyrimidines. J. Am. Chem. Soc., 80, 3449– 3457. Rollo, I. M. (1955). The mode of action of sulphonamides proguanil and pyrimethamine on Plasmodium gallinaceum. Br. J. Pharmac. Chemother., 10, 208– 214. Roth, B., Falco, E. A. & Hitchings, G. H. (1962). 5-Benzyl-2,4-diaminopyrimidines as antibacterial agents. I. Synthesis and antibacterial activity J. mednl. pharm. Chem., 5, 1103– 1123. Schneider, M., Schwarzenberg, L., Cattan, A., Schlumberger, J. R., Amiel, J. L. & Mathé, G. (1965). Essai de traitement de diverses infections a ‘Proteus’ par le 2,4 diamino 5(3,4,5 triméthoxybelzyl) pyrimidine, ou (trimethoprim). Presse med., 73, 893– 894. Sourander, L. B. & Werner, G. E. (1967). Efficacy and tolerance of sulphonamide trimethoprim combinations in geriatric patients with bactiuria. Proceedings 5th International Congress of Chemotherapy Vienna June 2. Thiersch, J. B. (1963). The effect of substituted 2,4 diaminopyrimidines on the rat fetus in utero. 3rd International Congress of Chemotherapy, International Society of Chemotherapy, Stuttgart, Germany, 367– 372. Wood, R. C., Geltzer, A. & Hitchings, G. H. (1960). Comparative effects of various antimetabolites on growth and synthesis of citrovorum factor by Streptococcus faecalis. J. Bact., 79, 306– 307. Wood, R. C. & Hitchings, G. H. (1959). A study of the uptake and degradation of folic acid, citrovorum factor, aminopterin, and pyrimethamine by bacteria. J. biol. Chem., 234, 2381– 2385. Zbinden, G. (1964). Molecular modifications in the development of newer anti-infective agents. Molecular Modifications in Drug Design, ed. R. F. Gould, p. 25. Washington, D.C.: American Chemical Society. Citing Literature Volume33, Issue1May 1968Pages 72-90 ReferencesRelatedInformation

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