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Chemical Compound Review:

CCRIS 6841 3-(1-methyl-5-nitro-imidazol- 2-yl)-3a,4,5...

Synonyms: Mk-436, SureCN11541878, MK-0436, AC1L3OHT, LS-33636, ...

Andrade, S.G. et al., Teixeira, A.R. et al., Gutteridge, W.E. et al., Jennings, F.W., Vandenheuvel, W.J. et al.

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Disease relevance of MK 436

Benznidazole cleared up parasitaemias in the shortest time and was associated with 41.6 per cent of lymphoma growths, whereas MK-436 required twice as much time to clear blood parasites, and showed lymphomas in 25 per cent of experimental rabbits [1].
The latter combination of MK 436 and Mel Cy, producing a rapid cure of CNS trypanosomiasis with only a two dose regimen and thus, would make an ideal universal treatment for both early- and late-stage trypanosomiasis [2].
Mice infected with the Colombian strain and treated with MK-436, was parasitologically cured in 5/6 cases and showed mild inflammatory infiltration and fibrosis [3].

High impact information on MK 436

Crithidia fasciculata, which contains high levels of a cytosolic catalase, is sensitive to inhibition by at least two nitroheterocyclic drugs, Nifurtimox and MK 436, both of which are also active against Trypanosoma cruzi [4].
This investigation was performed to verify the effect of specific chemotherapy (Benznidazole or MK-436) on the inflammatory and fibrotic cardiac alterations in mice chronically infected with the strains 21 SF (Type II) and Colombian (Type III) of Trypanosoma cruzi [3].

Analytical, diagnostic and therapeutic context of MK 436

Metabolite fractions from the urine of a dog dosed with 3a,4,5,6,7a-hexahydro-3-(1-methyl-5-nitro-1H-imidazol-2-yl)-1,2-benzisoxazole (MK-0436) were obtained by the use of high-performance liquid chromatography [5].

References

Malignant, non-Hodgkin's lymphomas in Trypanosoma cruzi-infected rabbits treated with nitroarenes. Teixeira, A.R., Silva, R., Cunha Neto, E., Santana, J.M., Rizzo, L.V. J. Comp. Pathol. (1990) [Pubmed]
Combination chemotherapy of CNS trypanosomiasis. Jennings, F.W. Acta Trop. (1993) [Pubmed]
Reversibility of cardiac fibrosis in mice chronically infected with Trypanosoma cruzi, under specific chemotherapy. Andrade, S.G., Stocker-Guerret, S., Pimentel, A.S., Grimaud, J.A. Mem. Inst. Oswaldo Cruz (1991) [Pubmed]
Crithidia fasciculata: a catalase-containing trypanosomatid sensitive to nitroheterocyclic drugs. Gutteridge, W.E., Ross, J., Hargadon, M.R., Hudson, J.E. Trans. R. Soc. Trop. Med. Hyg. (1982) [Pubmed]
Identification of canine urinary metabolites of the antiprotozoal agent 3a,4,5,6,7,7a-hexahydro-3-(1-methyl-5-nitro-1H-imidazol-2-yl)-1,2-benzisoxazole . Vandenheuvel, W.J., Onofrey, D., Zweig, J.S., Pile, J., Kirkman-Bey, N., Arison, B.H. Journal of pharmaceutical sciences. (1980) [Pubmed]

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