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Chemical Compound Review

DO870     (2R)-2-(2,4-difluorophenyl)- 1-[3-[(Z)-2-[4...

Synonyms: AC1O5LAB, LS-186886, LS-187540, D-0870, Ici 195739, ...
 
 
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Disease relevance of ZD0870

  • We investigated the in-vitro antiproliferative effects and mechanism of action of both enantiomers of the bis-triazole derivative ICI 195,739 against epimastigotes and amastigotes of Trypanosoma cruzi, the aetiological agent of Chagas' disease [1].
 

High impact information on ZD0870

 

Analytical, diagnostic and therapeutic context of ZD0870

  • ICI 195,739 shows superior potency to other azoles in eliminating vaginal candidosis or dermatophyte infections in animal models of infection by both oral dosing and topical application; effective doses are in the range of 0.5-5.0 mg/kg/day or 0.01-0.30% in a topical formulation [5].

References

  1. In-vitro antiproliferative effects and mechanism of action of the bis-triazole D0870 and its S(-) enantiomer against Trypanosoma cruzi. Liendo, A., Lazardi, K., Urbina, J.A. J. Antimicrob. Chemother. (1998) [Pubmed]
  2. Experimental chemotherapy with combinations of ergosterol biosynthesis inhibitors in murine models of Chagas' disease. Maldonado, R.A., Molina, J., Payares, G., Urbina, J.A. Antimicrob. Agents Chemother. (1993) [Pubmed]
  3. Synthesis and structure-activity relationships of a novel antifungal agent, ICI 195,739. Boyle, F.T., Gilman, D.J., Gravestock, M.B., Wardleworth, J.M. Ann. N. Y. Acad. Sci. (1988) [Pubmed]
  4. Biochemical mode of action and enantiomeric selectivity of SDZ 89-485, a new triazole antimycotic. Ryder, N.S. J. Med. Vet. Mycol. (1990) [Pubmed]
  5. Activity of ICI 195,739--a novel, orally active bistriazole--in rodent models of fungal and protozoal infections. Ryley, J.F., McGregor, S., Wilson, R.G. Ann. N. Y. Acad. Sci. (1988) [Pubmed]
 
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