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Chemical Compound Review

Saperconazol     2-butan-2-yl-4-[4-[4-[4- [[(2R,4R)-2-(2,4...

Synonyms: SAPERCONAZOLE, Saperconazolum, SureCN1650334, RWJ-27758, AC1L1TAK, ...
 
 
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Disease relevance of AIDS008523

 

High impact information on AIDS008523

  • The efficacy of a new triazole antifungal agent, saperconazole, in a murine model of disseminated candidiasis was studied [2].
  • RESULTS: Removal of 25% of the corneal epithelium produced an increase in corneal saperconazole concentration compared with eyes with intact epithelium [5].
  • When inhibition of the growth of Acanthamoeba was the only parameter used to measure the effectiveness of these drugs, saperconazole was found to be most active with IC50 (concentration of drug that inhibited by 50%, the growth of A. polyphaga trophozoites incubated at 28 degrees C for 48 h) of 0.95 microM [6].
  • Ocular pharmacokinetics of saperconazole in rabbits. A potential agent against keratomycoses [7].
  • Following a single 20-microL drop of 0.25% saperconazole in normal corneas, a mean (+/- SEM) peak level of 2.32 +/- 0.06 micrograms/g was achieved in 10 minutes [7].
 

Anatomical context of AIDS008523

 

Associations of AIDS008523 with other chemical compounds

 

Gene context of AIDS008523

 

Analytical, diagnostic and therapeutic context of AIDS008523

References

  1. Saperconazole therapy in a rabbit model of invasive aspergillosis. Patterson, T.F., George, D., Miniter, P., Andriole, V.T. Antimicrob. Agents Chemother. (1992) [Pubmed]
  2. Saperconazole therapy of murine disseminated candidiasis: efficacy and interactions with amphotericin B. Sugar, A.M., Salibian, M., Goldani, L.Z. Antimicrob. Agents Chemother. (1994) [Pubmed]
  3. Saperconazole in the treatment of systemic and subcutaneous mycoses. Franco, L., Gomez, I., Restrepo, A. International journal of dermatology. (1992) [Pubmed]
  4. Clinical efficacy and tolerability of saperconazole for tinea of glabrous skin. A report on four cases. Zienicke, H., Korting, H.C. Mycoses (1993) [Pubmed]
  5. The relationship of corneal epithelial defect size to drug penetration. Johnson, D.A., Johns, K.J., Robinson, R.D., Head, W.S., O'Day, D.M. Arch. Ophthalmol. (1995) [Pubmed]
  6. In vitro assessment of susceptibility of Acanthamoeba polyphaga to drugs using combined methods of dye-binding assay and uptake of radiolabelled adenosine. Asiri, S., Ogbunude, P.O., Warhurst, D.C. Int. J. Parasitol. (1994) [Pubmed]
  7. Ocular pharmacokinetics of saperconazole in rabbits. A potential agent against keratomycoses. O'Day, D.M., Head, W.S., Robinson, R.D., Williams, T.E., Wolff, R. Arch. Ophthalmol. (1992) [Pubmed]
  8. A preliminary study of in vitro antibiotic activity of saperconazole and other azoles on Paracoccidioides brasiliensis. San-Blas, G., Calcagno, A.M., San-Blas, F. J. Med. Vet. Mycol. (1993) [Pubmed]
  9. Efficacy of oral saperconazole in systemic murine aspergillosis. Hanson, L.H., Clemons, K.V., Denning, D.W., Stevens, D.A. J. Med. Vet. Mycol. (1995) [Pubmed]
  10. In vitro and in vivo antidermatophytic activity of saperconazole, a new fluorinated triazole. Fu, K.P., Isaacson, D.M., Lococo, J., Foleno, B., Hilliard, J. Drugs under experimental and clinical research. (1992) [Pubmed]
  11. In vitro activity of saperconazole (R66 905) compared with amphotericin B and itraconazole against Aspergillus species. Denning, D.W., Hanson, L.H., Stevens, D.A. Eur. J. Clin. Microbiol. Infect. Dis. (1990) [Pubmed]
  12. In vitro antifungal activity of saperconazole (R 66905) against Candida and Torulopsis. Mallié, M., Montès, B., Lebecq, J.C., Bastide, J.M. Mycoses (1989) [Pubmed]
  13. Saperconazole: a selective inhibitor of the cytochrome P-450-dependent ergosterol synthesis in Candida albicans, Aspergillus fumigatus and Trichophyton mentagrophytes. Vanden Bossche, H., Marichal, P., Willemsens, G., Bellens, D., Gorrens, J., Roels, I., Coene, M.C., Le Jeune, L., Janssen, P.A. Mycoses (1990) [Pubmed]
  14. Evaluation of himachalol in murine invasive aspergillosis. Chowdhry, L., Khan, Z.K., Kulshrestha, D.K. Mycoses (1996) [Pubmed]
 
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