R66905 - CAS 110588-57-3
Category: Inhibitor
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Molecular Formula:
Molecular Weight:
R66905, also known as saperconazole, is a broad-spectrum antifungal triazole.
Saperconazole; SPZ; R66905; R-66905; R 66905; 2-butan-2-yl-4-[4-[4-[4-[[(2R,4S)-2-(2,4-difluorophenyl)-2-(1,2,4-triazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy]phenyl]piperazin-1-yl]phenyl]-1,2,4-triazol-3-one; saperconazole
Store in a cool and dry place (or refer to the Certificate of Analysis).
Boiling Point:
812.5±75.0 ℃ at 760 Torr
Melting Point:
189.5 ℃
1.37±0.1 g/cm3
Canonical SMILES:
1.Saperconazole: in vitro and in vivo anticandidal activity.
Fu KP;Isaacson D;Foleno B;LoCoco J Chemotherapy. 1992;38(3):174-8.
The in vitro activity of saperconazole against eight candidal species (81 strains) was determined and compared with fluconazole, Sch 39304 and amphotericin B. Using brain heart infusion broth with an inoculum of 10(4) CFU/ml, the MIC ranges (micrograms/ml) of saperconazole were: less than or equal to 0.015- greater than 32 for Candida albicans, less than or equal to 0.015-16 for C. tropicalis, less than or equal to 0.015-32 for C. glabrata, less than or equal to 0.015-32 for C. parapsilosis, less than or equal to 0.015-0.12 for C. guilliermondii and less than or equal to 0.015-0.06 for C. krusei. Saperconazole was the most active agent tested against Candida species. Saperconazole and 5-fluorocytosine combinations showed synergistic interactions against Candida species, and no antagonistic interaction was demonstrated. In a rat vaginal candidiasis infection model, saperconazole and fluconazole were equipotent producing 75-100% cures at levels of 0.016-0.25%, respectively, when dosed intravaginally. After single oral dosing, saperconazole was 5-fold more potent than fluconazole with an ED50 value of 0.53 mg/kg. These data demonstrate that saperconazole is effective in a rat vaginal candidiasis infection either with a single oral dose or by intravaginal treatment.
2.Treatment of tropical mycoses.
Restrepo A J Am Acad Dermatol. 1994 Sep;31(3 Pt 2):S91-102.
Several subcutaneous and deep-seated mycoses are either observed more frequently in the tropical areas or are restricted to certain regions within the tropics. These mycoses include sporotichosis, chromoblastomycosis, entomophthoromycosis, eumycetoma, lobomycosis, and paracoccidioidomycosis. In sporotrichosis and paracoccidioidomycosis, therapy often results in either complete resolution or marked improvement. For decades sporotrichosis has been treated successfully with potassium iodide, but recently the triazole compounds, especially itraconazole, have proved effective and free of major side effects. The usual therapy for paracoccidioidomycosis is sulfonamides or amphotericin B; the former requires prolonged treatment, whereas the latter causes a significant degree of toxicity. Various azole derivatives (ketoconazole, fluconazole, saperconazole, and itraconazole) allow shorter treatment courses, can be given orally, and are more effective. Presently, itraconazole is the drug of choice. Chromoblastomycosis is a difficult condition to treat, especially if it is caused by Fonsecaea pedrosoi. Several therapeutic approaches have been used, including heat, surgery, cryotherapy, thiabendazole, amphotericin B combined with flucytosine, and azole derivatives, but their success has been modest.
3.Effects of cytochrome P-450 inhibitors on the in vivo metabolism of all-trans-retinoic acid in rats.
Van Wauwe JP;Coene MC;Goossens J;Cools W;Monbaliu J J Pharmacol Exp Ther. 1990 Jan;252(1):365-9.
This study examines the effects of ketoconazole, R 75 251 and some other cytochrome P-450 inhibitors on the in vivo metabolism of all-trans-retinoic acid (RA) in normal rats. Oral treatment with ketoconazole or R 75 251 (40 mg/kg, -1 hr) reduced the elimination rate of i.v. injected RA from plasma: the half-life of RA increased from 27 min in control-treated animals to 43 min and 76 min after dosing with ketoconazole and R 75 251, respectively. However, neither drug had an effect on the distribution volume of the retinoid. Two hours after i.v. injection of RA, residual plasma levels of the retinoid were 11.2 ng/ml in ketoconazole and 22.7 ng/ml in R 75 251-treated rats. The other P-450 inhibitors, aminoglutethimide, cimetidine, itraconazole, metyrapone and saperconazole, showed no sparing effect on RA elimination: plasma levels of the acid were below 1 ng/ml, as in control-treated animals. Administration of ketoconazole or R 75 251 (40 mg/kg, -2 hr) to rats also enhanced endogenous plasma concentrations of RA. Levels of the retinoid were raised from mostly undetectable values (less than 0.5 ng/ml) to 1.3 +/- 0.1 and 2.5 0.1 ng/ml after treatment with ketoconazole and R 75 251, respectively.
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CAS 110588-57-3 R66905

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