No abstract available.
Candida* ; Fluconazole*

No abstract available.
Candidiasis* ; Fluconazole*

No abstract abailble.
Fluconazole* ; Sporotrichosis*

No abstract available.
Fluconazole* ; Humans

No abstract available.
Candidiasis, Oral* ; Fluconazole*

No abstract available.
Fluconazole* ; Tinea Capitis* ; Tinea*

No abstract available.
Candidiasis* ; Fluconazole* ; Humans

Fluconazol has been used as an effective antifungal drug for decades. However, increasing drug resistance make it becoming ineffective against many fungal strains. In search for new antifungal agents we have designed and synthesized eight derivatives of fluconazol, in which the hydroxy group of fluconazol was replaced by different functional groups, including halogens [Br (4a), Cl (4b), F (4c)}, azide (4d), cyanide (4e), carboxyl (4f), thiol (4g), and methanesulfonate (4h). Halogenated fluconazol derivatives (4a-4c) showed considerable antifungal activity against three fungal strains tested (C. albicans, A. niger, A. neoformans) with MIC values ranging from 139 to 552 mg/ml. Replacement of the -OH in fluconazol by bulkier groups like azide, cyanide, carboxyl, or methanesulfonate led to decrease or loss of antifungal activity. Exceptionally, however, a thiol derivative 4g (assigned UR/10289) exhibited very potent activity against all fungi tested, including two fluconazol-resistant strains (C. albicans, A. niger). This compound has been chosen as a candidate for further preclinical development by Parma Co. Ltd. (USA)
Fluconazole ; Pharmaceutical Preparations

BACKGROUND: Although standardized broth dilution methods for antifungal susceptibility testing are available, easier testing procedures are desirable. We evaluated the E-test (AB disk, Sweden) as a possible alternative instead of NCCLS (National Committee for Clinical Laboratory Standards) broth macrodilution method. METHODS: Fifty-two bloodstream isolates of Candida spp. (including 11 C. albicans, 13 C. tropicalis, 18 C. parapsilosis, 1 C. glabrata, 4 C. krusei, 2 C. pelliculosa, 2 C. lipolytica, and 1 C. guilliermondii) were tested. Amphotericin B and fluconazole MICs for each isolate were determined by both NCCLS broth macrodilution method and E-test. The results of E-test for Candida spp. were compared with those of NCCLS macrodilution method. For selecting plating media for E-test, we compared E-test results in two different media (RPMI and Casiton medium) using five ATCC Candida strains. RESULTS: As E-test media, we selected RPMI medium for amphotericin B and Casitone medium for fluconazole because of higher agreement with NCCLS method. The E-test and NCCLS method of 52 Candida spp. yielded a very narrow range of MICs (0.064-2.0 microgram/mL) for amphotericin B and a broad range of MICs (0.5-64 microgram/mL) for fluconazole. The agreements of E-test within one doubling dilutions of the macrodilution reference were 90.4% (24h and 48h) for amphotericin B, and 90.4% (24h) and 96.2% (48h) for fluconazole. CONCLUSION: The E-test is a valuable alternative to the NCCLS macrodilution method for amphotericin B and fluconazole susceptibility testing of Candida species.
Amphotericin B ; Candida* ; Fluconazole

BACKGROUND: Although the broth microdilution method has been recently established for antifungal susceptibility testing of the Candida species, there is still an argue in the interpretation of the trailing endpoint. We evaluated the spectrophotometric broth microdilution method (SBM) to determine the fluconazole MICs from five different Candida species. METHODS: A total of 252 clinical isolates of five Candida species (144 C. albicans, 42 C. tropicalis, 32 C. glabrata, 28 C. parapsilosis, and 6 C. krusei) were tested for fluconazole susceptibility with the broth microdilution method. The MICs were spectrophotometrically determined at 80% (Spec-80%) and 50% (Spec-50%) decrease in absorbance as compared with growth control, respectively. The results were compared with the fluconazole MICs tested by the National Committee for the Clinical Laboratory Standards (NCCLS) macrodilution method. RESULTS: When MICs were obtained by Spec-80%, the agreements of SBM and the NCCLS macro dilution method within two doubling dilutions were 92.4% (220/238) at 24 h and 78.6% (198/252) at 48 h for all Candida species. Using the Spec-50%, those were increased to 97.9% (233/238) at 24 h and 98.8% (249/252) at 48 h (P<0.01). Especially, for C. albicans and C. tropicalis, the agreement of the Spec-50% was significantly higher than those of the Spec-80% at 48 h; 97.9% vs. 75.0%, for C. albicans (P<0.01), and 100% vs. 57.1%, for C. tropicalis (P<0.01). CONCLUSIONS: These data suggest that the SBM using Spec-50% can provide a more precise and objective mean for fluconazole susceptibility testing, especially for C. albicans and C. tropicalis.
Candida albicans ; Candida* ; Fluconazole*