Hostname: page-component-848d4c4894-jbqgn Total loading time: 0 Render date: 2024-06-17T21:08:09.489Z Has data issue: false hasContentIssue false

The action of 2:4-diamino-6:7-diisopropylpteridine upon Plasmodium gallinaceum and its relation to other compounds which are pteroylglutamic acid antagonists

Published online by Cambridge University Press:  06 April 2009

Ann Bishop
Affiliation:
Molteno Institute, University of Cambridge

Extract

1. Two strains of Plasmodium gallinaceum were made resistant to 2:4-diamino-6:7-diisopropylpteridine (0/129) by treatment with that drug.

2. The 0/129-resistant strains were resistant to proguanil, pyrimethamine, 2:4-diamino-6:7-diphenylpteridine (0/63) and 2:4-diamino-5-(p–chlorophenoxy)-6-methylpyrimidine (48–210), but not to sulphadiazine.

3. In one strain treated with 0/129, the development of resistance to that drug itself preceded resistance to proguanil, and resistance to proguanil preceded resis tance to pyrimethamine.

4. A strain of P. gallinaceum made resistant to 0/63 was resistant to proguanil, pyrimethamine and 0/129, but not to sulphadiazine.

5. The action of 0/129 and proguanil upon P. gallinaceum was not antagonized by p–A.B., though in the minimum effective dose their action was antagonized by relatively large doses of P.G.A.

6. Whereas the action of sulphadiazine upon P. gallinaceum was antagonized competitively by p–A.B., it was antagonized by P.G.A. only when the sulphadiazine was given in small doses.

Type
Research Article
Copyright
Copyright © Cambridge University Press 1954

Access options

Get access to the full version of this content by using one of the access options below. (Log in options will check for institutional or personal access. Content may require purchase if you do not have access.)

References

REFERENCES

Angier, R. B., Boothe, J. H., Hutchings, B. L., Mowat, J. H., Semb, J., Stokstad, E. L. R., SubbaRow, Y., Waller, C. W., Cosulich, D. B., Fahrenbach, M. J., Hult-Quist, M. E., Kuh, E., Northey, E. H., Seeger, D. R. & Smith, J. M. (1946). The structure and synthesis of the liver L. casei factor. Science, 103, 667.CrossRefGoogle Scholar
Bishop, A. & Birkett, B. (1948). Drug-resistance in Plasmodium gallinaceum, and the persistence of paludrine-resistance after mosquito transmission. Parasitology, 39, 125.CrossRefGoogle ScholarPubMed
Bishop, A. & McConnachie, E. W. (1948). Resistance to sulphadiazine and ‘paludrine’ in the malaria parasite of the fowl (P. gallinaceum). Nature, Lond., 162, 541.CrossRefGoogle ScholarPubMed
Bishop, A. & McConnachie, E. W. (1950 a). Sulphadiazine-resistance in Plasmodium gallinaceum and its relation to other antimalarial compounds. Parasitology, 40, 163.CrossRefGoogle ScholarPubMed
Bishop, A. & McConnachie, E. W. (1950 b). Cross-resistance between sulphanilamide and paludrine (proguanil) in a strain of Plasmodium gallinaceum resistant to sulphanilamide. Parasitology, 40, 175.CrossRefGoogle Scholar
Bishop, A. & McConnachie, E. W. (1951). The inhibition by p–aminobenzoic acid of the development of paludrine-resistance as produced by sulphonamides in Plasmodium gallinaceum. Parasitology, 41, 105.CrossRefGoogle ScholarPubMed
Blanchard, K. C. (1941). The isolation of p–aminobenzoic acid from yeast. J. Biol. Chem. 140, 919.CrossRefGoogle Scholar
Campbell, N. R., Dunsmuir, J. H. & Fitzgerald, M. E. H. (1950). Antibacterial pteridines: 6:7-dialkyl derivatives of 2:4-diaminopteridine. J. Chem. Soc. p. 2743.CrossRefGoogle Scholar
Carrington, H. C., Crowther, A. F., Davey, D. G., Levi, A. A. & Rose, F. L. (1951). A metabolite of ‘Paludrine’ with high antimalarial activity. Nature, Lond., 168, 1080.CrossRefGoogle ScholarPubMed
Collier, H. O. J. & Waterhouse, P. D. (1950 a). Studies in the chemotherapy of cholera. II. In vitro vibriostatic properties of certain 2:4-diaminopteridines. Ann. Trop. Med. Parasit. 44, 156.CrossRefGoogle Scholar
Collier, H. O. J. & Waterhouse, P. D. (1950 b). Studies in the chemotherapy of cholera. Ann. Trop. Med. Parasit. 44, 273.CrossRefGoogle ScholarPubMed
Crowther, A. F. & Levi, A. A. (1953). Proguanil—the isolation of a metabolite of high antimalarial activity. Brit. J. Pharmacol. 8, 93.Google ScholarPubMed
Daniel, L. J., Norris, L. C., Scott, M. L. & Heuser, G. F. (1947). Growth inhibition of bacteria by synthetic pterins. I. Studies with Streptococcus faecalis, Lactobacillus casei, and Lactobacillus arabinosus. J. Biol. Chem. 169, 689.CrossRefGoogle ScholarPubMed
Falco, E. A., Goodwin, L. G., Hitchings, G. H., Rollo, I. M. & Russell, P. B. (1951). 2:4-Diaminopyrimidines—a new series of antimalarials. Brit. J. Pharmacol. 6, 185.Google ScholarPubMed
Greenberg, J. (1949 a). The antimalarial activity of 2:4-diamino-6, 7-diphenylpterin; its potentiation by sulfadiazine and inhibition by pteroylglutamic acid. J. Pharmacol. 97, 484.Google Scholar
Greenberg, J. (1949 b). Inhibition of the antimalarial activity of chlorguanide by pteroylglutamic acid. Proc. Soc. Exp. Biol., N.Y., 71, 306.CrossRefGoogle ScholarPubMed
Greenberg, J. (1949 c). The potentiation of the antimalarial activity of chlorguanide by p–aminobenzoic acid competitors. J. Pharmacol. 97, 238.Google ScholarPubMed
Greenberg, J. (1953). Reversal of the activity of chlorguanide against Plasmodium gallinaceum by free or conjugated p–aminobenzoic acid. Exp. Parasitol. 2, 271.CrossRefGoogle Scholar
Greenberg, J. & Richeson, E. M. (1950). Potentiation of the antimalarial activity of sulfadiazine by 2, 4-diamino-5-aryloxypyrimidines. J. Pharmacol. 99, 444.Google ScholarPubMed
Greenberg, J. & Richeson, E. M. (1951). Effect of 2, 4-diamino-5-(p–chlorophenoxy)-6-methylpyrimidine and 2, 4-diamino-6, 7-diphenylpteridine on chlorguanide-resistant strain of Plasmodium gallinaceum. Proc. Soc. Exp. Biol., N.Y., 77, 174.CrossRefGoogle Scholar
Greenberg, J., Boyd, B. L. & Josephson, E. S. (1948). Synergistic effect of chlorguanide and sulfadiazine against Plasmodium gallinaceum in the chick. J. Pharmacol. 94, 60.Google ScholarPubMed
Hitchings, G. H. (1952). Daraprim as an antagonist of folio and folinic acids. Trans. R. Soc. Trop. Med. Hyg. 46, 467.CrossRefGoogle Scholar
Hitchings, G. H., Falco, E. V., Vanderwerff, H., Russell, P. B. & Elion, G. B. (1952). Antagonists of nucleic acid derivatives. VII. 2, 4-diaminopyrimidines. J. Biol. Chem. 199, 43.CrossRefGoogle ScholarPubMed
Jones, S. A. (1953). Experiments to determine if a proguanil-resistant strain of P. falciparum would respond to large doses of pyrimethamine. Brit. Med. J. p. 977.CrossRefGoogle Scholar
Lampden, J. O. & Jones, M. J. (1946 a). The antagonism of sulfonamides by pteroylglutamic acid and related compounds. J. Biol. Chem. 164, 485.CrossRefGoogle Scholar
Lampden, J. O. & Jones, M. J. (1946 b). The antagonism of sulfonamide inhibition of certain lactobacilli and enterococci by pteroylglutamic acid and related compounds. J. Biol. Chem. 166, 435.CrossRefGoogle Scholar
McConnachie, E. W. (1953). The action of 2:4-diamino-6:7-diisopropylpteridine on normal, proguanil-and sulphadiazine-resistant strains of Plasmodium gallinaceum. Parasitology, 42, 272.CrossRefGoogle Scholar
Maier, J. & Riley, E. (1942). Inhibition of antimalarial action of sulfonamides by p–aminobenzoic acid. Proc. Soc. Exp. Biol., N.Y., 50, 152.CrossRefGoogle Scholar
Marshall, E. K., Litchfield, J. T. & White, H. J. (1942). Sulfonamide therapy of malaria in ducks. J. Pharmacol. 75, 89.Google Scholar
Mills, R. C., Briggs, G. M., Luckey, T. D. & Elvehjem, C. A. (1944). Production of unidentified vitamins by a strain of Mycobacterium tuberculosis grown on synthetic medium with p–aminobenzoic acid. Proc. Soc. Exp. Biol., N.Y., 56, 240.CrossRefGoogle Scholar
Robertson, G. I., Davey, D. G. & Fairley, H. N. (1952). Cross-resistance between ‘Daraprim’ and proguanil. Brit. med. J. 2, 1255.CrossRefGoogle Scholar
Rollo, I. M. (1951). A 2:4-diamino pyrimidine in the treatment of proguanil-resistant laboratory malarial strains. Nature, Lond., 168, 333.CrossRefGoogle Scholar
Rollo, I. M. (1952). Daraprim—experimental chemotherapy. Trans. R. Soc. Trop. Med. Hyg. 46, 474.CrossRefGoogle ScholarPubMed
Rubbo, S. D. & Gillespie, J. M. (1940). Para-amino benzoic acid as a bacterial growth factor. Nature, Lond., 146, 838.CrossRefGoogle Scholar
Sarett, H. P. (1947). Interrelationship between p–aminobenzoic acid and pteroylglutamic acid as growth factors for lactobacilli. J. Biol. Chem. 171, 265.CrossRefGoogle Scholar
Schmidt, L. H. & Genther, C. S. (1952). The antimalarial properties of 2, 4-diamino-5-p–chlorophenyl-6-ethylpyrimidine (Daraprim). J. Pharmacol. 107, 61.Google Scholar
Selbie, F. R. (1940). The inhibition of the action of sulphanilamide in mice by p–aminobenzoic acid. Brit. J. Exp. Path. 21, 90.Google Scholar
Singh, J., Ray, A. P., Basu, P. C. & Nair, C. P. (1952). Acquired resistance to proguanil in Plasmodium knowlesi. Trans. R. Soc. Trop. Med. Hyg. 46, 639.CrossRefGoogle ScholarPubMed
Thurston, J. P. (1950). Action of proguanil on P. berghei. Inhibition by p–aminobenzoic acid. Lancet, ii, 438.CrossRefGoogle Scholar
Thurston, J. P. (1953 a). Plasmodium berghei. Exp. Parasitol. 2, 311.CrossRefGoogle Scholar
Thurston, J. P. (1953 b). The chemotherapy of Plasmodium berghei. I. Resistance to drugs. Parasitology, 43, 246.CrossRefGoogle ScholarPubMed
Thurston, J. P. (1954). Chemotherapy of Plasmodium berghei. II. Antagonism of the action of drugs. Parasitology, 44, 99.CrossRefGoogle ScholarPubMed
Woods, D. D. (1940). The relation of p–aminobenzoic acid to the mechanism of the action of sulphanilamide. Brit. J. Exp. Path. 21, 74.Google Scholar