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Chemical Compound Review

Rochagan     N-benzyl-2-(2-nitroimidazol- 1-yl)ethanamide

Synonyms: Radanil, Ragonil, Benznidazol, BENZNIDAZOLE, benzonidazol, ...
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Disease relevance of Radanil

  • Should benznidazole be used in chronic Chagas' disease [1]?
  • T cruzi parasitemias detected on three occasions were successfully treated with benzonidazole [2].
  • Again, however, benznidazole did not produce a consistently greater therapeutic gain than MISO because it also enhanced normal tissue toxicity while MISO did not [3].
  • The present studies compared the potential therapeutic benefit of combining MISO (partition coefficient, 0.43) or benznidazole (BENZO) (partition coefficient, 8.5) in KHT sarcoma or RIF-1 tumor-bearing C3H mice [4].
  • The results indicated that in immunocompetent animals SCH 56592 at 20 mg/kg of body weight/day provided protection (80 to 90%) against death caused by all strains, a level comparable or superior to that provided by the optimal dose of benznidazole (100 mg/kg/day) [5].

High impact information on Radanil

  • The advantage of benznidazole over MISO was lost, however, because benznidazole gave more toxicity in the normal tissues than MISO [3].
  • In experiments where the nitroimidazoles were administered by multiple small injections to maintain a blood plasma level between 50 and 100 micrograms/ml, benznidazole was also more effective than MISO in enhancing CCNU cytotoxicity in the tumors [3].
  • In murine macrophages, inducible NO synthase II (NOSII) gene expression is promoted at a transcriptional level by LPS and/or IFN-gamma with benznidazole (BZL), a trypanocidal drug, acting to down-regulate NOSII gene induction and hence inhibiting NO production [6].
  • Trypanocidal drug benznidazole impairs lipopolysaccharide induction of macrophage nitric oxide synthase gene transcription through inhibition of NF-kappaB activation [6].
  • We have investigated the influences of gamma interferon (IFN-gamma) and interleukin-12 (IL-12) on the efficacy of posaconazole (POS) treatment of acute experimental infections with Trypanosoma cruzi; the standard drug, benznidazole (BZ), was used as a positive control [7].

Chemical compound and disease context of Radanil


Biological context of Radanil


Anatomical context of Radanil

  • In this present work, we decided to evaluate the impact of benznidazole treatment upon the thymus involution following acute T. cruzi infection in mice [12].
  • Benznidazole treatment following acute Trypanosoma cruzi infection triggers CD8+ T-cell expansion and promotes resistance to reinfection [16].
  • However, little is known about the impact of benznidazole (N-benzyl-2-nitroimidazole acetamide), the drug available for clinical treatment of the infection, on the immune system in the infected host [16].
  • In Vero cells infected with amastigotes, 25 muM BSO was able to potentiate the effect of nifurtimox and benznidazole as measured by the percentage of infected Vero cells multiplied by the average number of intracellular amastigotes (endocytic index) [17].
  • Using C3H/He mouse liver microsomes and KHT tumour homogenates, we have investigated the effects of temperature (33-44 degrees) on the anaerobic nitroreduction of benznidazole (BENZO) to its amine metabolite in vitro [18].

Associations of Radanil with other chemical compounds


Gene context of Radanil

  • These results suggest that activation of the immune system by the parasite and endogenous interferon-gamma play a major role in the efficacy of benznidazole against infection with T. cruzi [23].
  • Sera collected during the longitudinal follow-up of benznidazole-treated acutely and congenitally infected patients became negative for T. cruzi as determined by tests presently used to assess cure; however, the sera remained positive for T. cruzi by the trans-sialidase inhibition assay (TIA) up to 14 years after treatment [24].
  • These results demonstrate that treatment with benznidazole in the chronic phase of infection prevents the development of severe chronic cardiomyopathy, despite the lack of complete parasite eradication [25].
  • The levels of antibodies against T. cruzi antigens (epimastigote extract, P2beta, and trans-sialidase) as well as antibodies against peptides of the second extracellular loops of beta1-adrenergic and M2-muscarinic cardiac receptors were also lower in the sera from benznidazole-treated mice than in the sera from untreated mice [25].
  • Deletion of the Trypanosoma brucei Superoxide Dismutase Gene sodb1 Increases Sensitivity to Nifurtimox and Benznidazole [26].

Analytical, diagnostic and therapeutic context of Radanil


  1. Should benznidazole be used in chronic Chagas' disease? Bestetti, R.B. Lancet (1997) [Pubmed]
  2. Heart transplantation in Chagas' disease. 10 years after the initial experience. de Carvalho, V.B., Sousa, E.F., Vila, J.H., da Silva, J.P., Caiado, M.R., Araujo, S.R., Macruz, R., Zerbini, E.J. Circulation (1996) [Pubmed]
  3. Effect of partition coefficient on the ability of nitroimidazoles to enhance the cytotoxicity of 1-(2-chloroethyl)-3-cyclohexyl-1-nitrosourea. Hirst, D.G., Brown, J.M., Hazlehurst, J.L. Cancer Res. (1983) [Pubmed]
  4. In vivo potentiation of 1-(2-chloroethyl)-3-cyclohexyl-1-nitrosourea by the radiation sensitizer benznidazole. Siemann, D.W., Morrissey, S., Wolf, K. Cancer Res. (1983) [Pubmed]
  5. Activities of the triazole derivative SCH 56592 (posaconazole) against drug-resistant strains of the protozoan parasite Trypanosoma (Schizotrypanum) cruzi in immunocompetent and immunosuppressed murine hosts. Molina, J., Martins-Filho, O., Brener, Z., Romanha, A.J., Loebenberg, D., Urbina, J.A. Antimicrob. Agents Chemother. (2000) [Pubmed]
  6. Trypanocidal drug benznidazole impairs lipopolysaccharide induction of macrophage nitric oxide synthase gene transcription through inhibition of NF-kappaB activation. Piaggio, E., Sancéau, J., Revelli, S., Bottasso, O., Wietzerbin, J., Serra, E. J. Immunol. (2001) [Pubmed]
  7. The Anti-Trypanosoma cruzi Activity of Posaconazole in a Murine Model of Acute Chagas' Disease Is Less Dependent on Gamma Interferon than That of Benznidazole. Ferraz, M.L., Gazzinelli, R.T., Alves, R.O., Urbina, J.A., Romanha, A.J. Antimicrob. Agents Chemother. (2007) [Pubmed]
  8. Antibacterial activities of the antiparasitic drugs nifurtimox and benznidazole. Hof, H. Antimicrob. Agents Chemother. (1989) [Pubmed]
  9. Proinflammatory and cytotoxic effects of hexadecylphosphocholine (miltefosine) against drug-resistant strains of Trypanosoma cruzi. Saraiva, V.B., Gibaldi, D., Previato, J.O., Mendonça-Previato, L., Bozza, M.T., Freire-De-Lima, C.G., Heise, N. Antimicrob. Agents Chemother. (2002) [Pubmed]
  10. A phase II study of CCNU with benznidazole for metastatic malignant melanoma. Bleehen, N.M., Roberts, J.T., Newman, H.F. Int. J. Radiat. Oncol. Biol. Phys. (1986) [Pubmed]
  11. A combination of benznidazole and ketoconazole enhances efficacy of chemotherapy of experimental Chagas' disease. Araújo, M.S., Martins-Filho, O.A., Pereira, M.E., Brener, Z. J. Antimicrob. Chemother. (2000) [Pubmed]
  12. Benznidazole therapy in Trypanosoma cruzi-infected mice blocks thymic involution and apoptosis of CD4+CD8+ double-positive thymocytes. Olivieri, B.P., Farias-De-Oliveira, D.A., Araujo-Jorge, T.C., Cotta-de-Almeida, V. Antimicrob. Agents Chemother. (2005) [Pubmed]
  13. Chemotherapy with benznidazole and itraconazole for mice infected with different Trypanosoma cruzi clonal genotypes. Toledo, M.J., Bahia, M.T., Carneiro, C.M., Martins-Filho, O.A., Tibayrenc, M., Barnabé, C., Tafuri, W.L., de Lana, M. Antimicrob. Agents Chemother. (2003) [Pubmed]
  14. Preclinical pharmacokinetics of benznidazole. Workman, P., White, R.A., Walton, M.I., Owen, L.N., Twentyman, P.R. Br. J. Cancer (1984) [Pubmed]
  15. The pharmacokinetics in mice and dogs of nitroimidazole radiosensitizers and chemosensitizers more lipophilic than misonidazole. White, R., Workman, P., Owen, L. Int. J. Radiat. Oncol. Biol. Phys. (1982) [Pubmed]
  16. Benznidazole treatment following acute Trypanosoma cruzi infection triggers CD8+ T-cell expansion and promotes resistance to reinfection. Olivieri, B.P., Cotta-De-Almeida, V., Araújo-Jorge, T. Antimicrob. Agents Chemother. (2002) [Pubmed]
  17. Buthionine sulfoximine increases the toxicity of nifurtimox and benznidazole to Trypanosoma cruzi. Faundez, M., Pino, L., Letelier, P., Ortiz, C., López, R., Seguel, C., Ferreira, J., Pavani, M., Morello, A., Maya, J.D. Antimicrob. Agents Chemother. (2005) [Pubmed]
  18. Heat-stimulated nitroreductive bioactivation of the 2-nitroimidazole benznidazole in vitro. Walton, M.I., Bleehen, N.M., Workman, P. Biochem. Pharmacol. (1987) [Pubmed]
  19. Misonidazole and benznidazole inhibit hydroxylation of CCNU by mouse liver microsomal cytochrome P-450 in vitro. Lee, F.Y., Workman, P., Cheeseman, K.H. Biochem. Pharmacol. (1987) [Pubmed]
  20. Cytochrome P-450, reductive metabolism, and cell injury. De Groot, H., Sies, H. Drug Metab. Rev. (1989) [Pubmed]
  21. Molecular enzymology of the reductive bioactivation of hypoxic cell cytotoxins. Walton, M.I., Wolf, C.R., Workman, P. Int. J. Radiat. Oncol. Biol. Phys. (1989) [Pubmed]
  22. Inhibition of Trypanosoma cruzi and T. brucei NADH fumarate reductase by benznidazole and anthelmintic imidazole derivatives. Turrens, J.F., Watts, B.P., Zhong, L., Docampo, R. Mol. Biochem. Parasitol. (1996) [Pubmed]
  23. Experimental chemotherapy against Trypanosoma cruzi infection: essential role of endogenous interferon-gamma in mediating parasitologic cure. Romanha, A.J., Alves, R.O., Murta, S.M., Silva, J.S., Ropert, C., Gazzinelli, R.T. J. Infect. Dis. (2002) [Pubmed]
  24. Long-lasting antibodies detected by a trans-sialidase inhibition assay of sera from parasite-free, serologically cured chagasic patients. Leguizamón, M.S., Russomando, G., Luquetti, A., Rassi, A., Almirón, M., González-Cappa, S.M., Frasch, A.C., Campetella, O. J. Infect. Dis. (1997) [Pubmed]
  25. Treatment with benznidazole during the chronic phase of experimental Chagas' disease decreases cardiac alterations. Garcia, S., Ramos, C.O., Senra, J.F., Vilas-Boas, F., Rodrigues, M.M., Campos-de-Carvalho, A.C., Ribeiro-Dos-Santos, R., Soares, M.B. Antimicrob. Agents Chemother. (2005) [Pubmed]
  26. Deletion of the Trypanosoma brucei Superoxide Dismutase Gene sodb1 Increases Sensitivity to Nifurtimox and Benznidazole. Prathalingham, S.R., Wilkinson, S.R., Horn, D., Kelly, J.M. Antimicrob. Agents Chemother. (2007) [Pubmed]
  27. Randomised trial of efficacy of benznidazole in treatment of early Trypanosoma cruzi infection. de Andrade, A.L., Zicker, F., de Oliveira, R.M., Almeida Silva, S., Luquetti, A., Travassos, L.R., Almeida, I.C., de Andrade, S.S., de Andrade, J.G., Martelli, C.M. Lancet (1996) [Pubmed]
  28. Stimulation by localized tumor hyperthermia of reductive bioactivation of 2-nitroimidazole benznidazole in mice. Walton, M.I., Bleehen, N.M., Workman, P. Cancer Res. (1989) [Pubmed]
  29. Use of polymerase chain reaction to diagnose the fifth reported US case of autochthonous transmission of Trypanosoma cruzi, in Tennessee, 1998. Herwaldt, B.L., Grijalva, M.J., Newsome, A.L., McGhee, C.R., Powell, M.R., Nemec, D.G., Steurer, F.J., Eberhard, M.L. J. Infect. Dis. (2000) [Pubmed]
  30. PCR assay for monitoring Trypanosoma cruzi parasitemia in childhood after specific chemotherapy. Galvão, L.M., Chiari, E., Macedo, A.M., Luquetti, A.O., Silva, S.A., Andrade, A.L. J. Clin. Microbiol. (2003) [Pubmed]
  31. A randomized study of CCNU with and without benznidazole in the treatment of recurrent grades 3 and 4 astrocytoma. Report to the Medical Research Council by the Brain Tumor Working Party. Bleehen, N.M., Freedman, L.S., Stenning, S.P. Int. J. Radiat. Oncol. Biol. Phys. (1989) [Pubmed]
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