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Chemical Compound Review

Ambilhar     1-(5-nitro-1,3-thiazol-2- yl)imidazolidin-2...

Synonyms: Ambilar, Niridazol, Niridazole, Niridazolum, Nitridazole, ...
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Disease relevance of Ambilhar

  • We investigated the immunosuppressive effects of the standard antihelminthic regimen of niridazole (25 mg/kg/day for seven days) in five patients with schistosomiasis [1].
  • Suppression of delayed hypersensitivity in schistosome-infected patients by niridazole [1].
  • Although 15-minute skin reactions to schistosomal antigens remained unchanged, niridazole reduced or ablated positive 48-hour skin reactions to tuberculin (PPD), mumps and schistosome antigens in all patients tested six and 15 days after therapy began [1].
  • We report here further studies on the mechanism of this drug-induced suppression of cellular hypersensitivity; the data show that niridazole active serum does not block the production of migration inhibitory factor once it has been initiated [2].
  • The mutagenicity of niridazole for Salmonella typhimurium depends upon the enzymic reduction of the nitro function [3].

High impact information on Ambilhar


Chemical compound and disease context of Ambilhar


Biological context of Ambilhar

  • In both isogeneic (Sarcoma 1 in A/JAX mice) and allogeneic (Sarcoma 180 in C57BL/6 mice) mouse tumor systems, treatment of the tumor-bearing mice with niridazole, an antiprarasitic drug, known to be a potent suppressor of cell mediated but not humoral immunity caused enhancement of metastases to regional popliteal nodes [12].
  • Effect of genotype on mutagenicity of niridazole in nitroreductase-deficient bacteria [3].
  • The results are taken to indicate that the residual activity (4.4%) seen in the strain with a base substitution mutation reflects the activity of an enzyme with an amino acid substitution, while the basal level (0.19%) of activity indicates the action of a different nitroreductase with a low specificity for niridazole [3].
  • Relative importance of bacterial and mammalian nitroreductases for niridazole mutagenesis [13].
  • The response of niridazole nitroreductase-deficient bacteria to niridazole is reduced to 4.4 and 0.19% that exhibited by the enzyme-proficient parent strain when the deficiency is the result of a base substitution and frame-shift mutation, respectively [3].

Anatomical context of Ambilhar


Associations of Ambilhar with other chemical compounds

  • Niridazole given in a single oral dose of 100 mg/kg to guinea pigs sensitized to ortho-chlorobenzoyl chloride-bovine gamma-globulin (OCB-BGG) regularly abolished delayed cutaneous reactivity [16].
  • Drug combinations incorporating niridazole at a lower dosage or for a shorter period were less effective, and azathioprine and prednisolone on their own or used together prolonged graft survival only marginally in this model [18].
  • Oxamniquine and niridazole significantly increased the AHH activity in vivo and in vitro, while the antimonial drugs enhanced the enzyme activity only in vivo [19].
  • MtzS strains displayed the greatest sensitivity towards niridazole and satranidazole, the latter having the highest redox potential of the 5-nitroimidazoles [20].
  • Of the two antischistosomal agents tested, hycanthone yielded an increase of 20-fold in the number of micronuclei over control at 40 mg/kg administered i.p. for five days, while with niridazole no increase in micronuclei at several concentrations tested both by single and multiple injection was found [21].

Gene context of Ambilhar


Analytical, diagnostic and therapeutic context of Ambilhar


  1. Suppression of delayed hypersensitivity in schistosome-infected patients by niridazole. Webster, L.T., Butterworth, A.E., Mahmoud, A.A., Mngola, E.N., Warren, K.S. N. Engl. J. Med. (1975) [Pubmed]
  2. Two stages in lymphocyte mediator production by differential susceptibility to blockade using niridazole. Daniels, J.C., Fajardo, I., David, J.R. Proc. Natl. Acad. Sci. U.S.A. (1975) [Pubmed]
  3. Effect of genotype on mutagenicity of niridazole in nitroreductase-deficient bacteria. Speck, W.T., Blumer, J.L., Rosenkranz, E.J., Rosenkranz, H.S. Cancer Res. (1981) [Pubmed]
  4. Letter: Schistosomiasis, immunosuppression and niridazole. Higashi, G.I., Gheith, H., Farid, Z., Miner, W.F. N. Engl. J. Med. (1975) [Pubmed]
  5. Detection of mutagenic activity of metronidazole and niridazole in body fluids of humans and mice. Legator, M.S., Connor, T.H., Stoeckel, M. Science (1975) [Pubmed]
  6. Carcinogenic effects of niridazole on rodents infected with Schistosoma mansoni. Bulay, O., Urman, H., Clayson, D.B., Shubik, P. J. Natl. Cancer Inst. (1977) [Pubmed]
  7. In vitro susceptibilities of 40 Campylobacter fetus subsp. jejuni strains to niridazole and metronidazole. Freydière, A.M., Gille, Y., Tigaud, S., Vincent, P. Antimicrob. Agents Chemother. (1984) [Pubmed]
  8. In vitro and in vivo activities of nitazoxanide against Clostridium difficile. McVay, C.S., Rolfe, R.D. Antimicrob. Agents Chemother. (2000) [Pubmed]
  9. Eosinophilia following treatment of patients with schistosomiasis mansoni and Bancroft's filariasis. Ottesen, E.A., Weller, P.F. J. Infect. Dis. (1979) [Pubmed]
  10. Antibacterial activities of nitrothiazole derivatives. Hof, H., Zak, O., Schweizer, E., Denzler, A. J. Antimicrob. Chemother. (1984) [Pubmed]
  11. Influence of immunomodulators, niridazole and levamisole, on autoimmune murine thyroiditis. Vladutiu, A.O. Immunol. Lett. (1982) [Pubmed]
  12. Effects of the immunosuppressive drug niridazole in isogeneic and allogeneic mouse tumor systems in vivo. Deodhar, S.D., Lee, V.W., Chiang, T., Mahmoud, A.F., Watten, K.S. Cancer Res. (1976) [Pubmed]
  13. Relative importance of bacterial and mammalian nitroreductases for niridazole mutagenesis. Blumer, J.L., Friedman, A., Meyer, L.W., Fairchild, E., Webster, L.T., Speck, W.T. Cancer Res. (1980) [Pubmed]
  14. Niridazole suppression of experimental allergic encephalomyelitis in Lewis rats. Paterson, P.Y., Harvey, J.M., Webster, L.T. J. Immunol. (1977) [Pubmed]
  15. Niridazole, a potent long-acting suppressant of cellular hypersensitivity. III. Minimal suppression of antibody responses. Pelley, R.P., Pelley, R.J., Stavitsky, A.B., Mahmoud, A.A., Warren, K.S. J. Immunol. (1975) [Pubmed]
  16. Studies on the mechanism of suppression of delayed hypersensitivity by the antischistosomal compund niridazole. Daniels, J.C., Warren, K.S., David, J.R. J. Immunol. (1975) [Pubmed]
  17. Aerobic metabolism of niridazole by rat liver microsomes. Blumer, J.L., Novak, R.F., Lucas, S.V., Simpson, J.M., Webster, L.T. Mol. Pharmacol. (1979) [Pubmed]
  18. Prolonged allograft survival with niridazole, azathioprine, and prednisolone. Salaman, J.R., Bird, M., Godfrey, A.M., Jones, B., Millar, D., Miller, J. Transplantation (1977) [Pubmed]
  19. Modification of cytochrome P-450, NADPH-cytochrome c reductase and aryl hydrocarbon hydroxylase activities by schistosomicidal drugs. Mostafa, M.H., Swelem, S.M., Farag, H.F. Biochem. Pharmacol. (1989) [Pubmed]
  20. Redox potential and oxygen concentration as factors in the susceptibility of Helicobacter pylori to nitroheterocyclic drugs. Smith, M.A., Edwards, D.I. J. Antimicrob. Chemother. (1995) [Pubmed]
  21. An evaluation of the micronuclei test using triethylenemelamine, trimethylphosphate, hycanthone and niridazole. Weber, E., Bidwell, K., Legator, M.S. Mutat. Res. (1975) [Pubmed]
  22. Identification and purification of immunosuppressive activity in the urine of rats and a human patient treated with niridazole. Lucas, S.V., Daniels, J.C., Schubert, R.D., Simpson, J.M., Mahmoud, A.A., warren, K.S., David, J.R., Webster, L.T. J. Immunol. (1977) [Pubmed]
  23. Inhibition of human mixed lymphocyte reactions by sera and urine dialysates from niridazole-treated rats. Jones, B.M., Bird, M., Howells, M., Massey, P.R., Millar, D., Miller, J.J., Reeves, S., Salaman, J.R. Transplantation (1977) [Pubmed]
  24. Therapeutic activities of nitrothiazole derivatives in experimental infections with Salmonella typhimurium and Bacteroides fragilis. Hof, H., Eisenbarth, B., Denzler, A., Zak, O., Schweizer, E. J. Antimicrob. Chemother. (1985) [Pubmed]
  25. Immune complex nephropathy i schistosomiasis. Falcão, H.A., Gould, D.B. Ann. Intern. Med. (1975) [Pubmed]
  26. Inhibition of the mixed lymphocyte reaction by fractionated niridazole urine dialysate. Jones, B.M., Bird, M., Griffin, P.J., Massey, P.R., Millar, D.A., Miller, J.J., Reeves, S., Salaman, J.R. J. Immunol. (1979) [Pubmed]
  27. Serial observations of circulating immune complexes in patients with acute schistosomiasis. Hiatt, R.A., Ottesen, E.A., Sotomayor, Z.R., Lawley, T.J. J. Infect. Dis. (1980) [Pubmed]
  28. Comparative in vitro activities of niridazole and metronidazole against anaerobic and microaerophilic bacteria. Hof, H., Sticht-Groh, V., Müller, K.M. Antimicrob. Agents Chemother. (1982) [Pubmed]
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