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At least 19 recordsLinked to original sources
PubMed1979

In vitro synergy and antagonism of antifungal agents against yeast-like fungi.

Some antifungal agents have been tested qualitatively in various associations against species of Candida, Cryptococcus and Torulopsis. The method used was the channel test and the results are confirmed by comparison with the serial dilution test in agar. The antagonism in vitro with the combination of amphotericin B imidazole suggests that caution must be exercised before prescribing the antifungal drugs in combination for man. The frequent synergy of flucytosine with econazole is, however, encouraging because of the low toxicity of the 2 drugs. Under the limited conditions described, the combination of flucytosine and amphotericin B was not found synergistic but additive on the strains of C. albicans used in this study. This combination was found synergistic for a strain of C. parapsilosis and is useful for avoiding resistance to flucytosine.

Antifungal Agents↗
PubMed1979

An imidazole derivative (Econazole) as an antifungal agent in cell culture systems.

Econazole, an imidazole derivative, was tested as an antifungal agent in different cell culture systems. In comparison with Fungizone, Econazole has the following advantageous properties: higher stability, higher solubility, better antifungal activity against contaminants of cell cultures and a wider range between minimal inhibitory to cytotoxic concentration with Aspergillus fumigatus, Candida albicans and Penicillium sp., activity against gram-positive bacteria and lower price. Econazole exerts no antiviral effect and can therefore be used for virus isolation from heavily contaminated material. The antagonistic effect of serum on the antifungal effect of Econazole and Fungizone was comparable as was the inhibitory effect of both antimycotics on Mycoplasma growth. In view of the above mentioned properties Econazole lactic acid can be recommended as an antifungal agent for cell culture systems at a concentration of 1 microgram per ml.

Amphotericin B↗
PubMed1977

The effect of various antifungal agents on aflatoxin production and growth characteristics of Aspergillus parasiticus and Aspergillus flavus in liquid medium.

Various antifungal agents were added to a medium of 2% yeast extract-4% sucrose. Spores of a toxigenic strain of Aspergillus parasiticus were inoculated into the medium and incubated at 26 degrees C. for 10 days. Growth of the mold and aflatoxin formation were monitored every 48 hours during the experiment. Of the antifungal agents evaluated, propionic acid and crystal violet were the most effective compounds in retarding mold growth. Propionic acid was fungicidal at concentrations greater than 3.0 microgram/ml. whereas crystal violet exhibited a mold retarding activity at levels greater than 2,0 microgram/ml. Crystal violet retarded the growth rate of the mold during the initial stages of growth, however, this retardation was overcome after 10 days of incubation. Crystal violet also retarded aflatoxin production and sporulation of Aspergillus parasiticus; however, aflatoxin production was the most sensitive parameter. A survey involving 12 toxigenic isolates of A. parasiticus and A. flavus indicated that these species vary markedly in susceptibility to crystal violet.

Aflatoxins↗
PubMed1977

Antifungal agents.

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Antifungal Agents↗
PubMed1976

Clinical evaluation of clotrimazole. A broad-spectrum antifungal agent.

The efficacy and safety of the broad-spectrum, topically applied antifungal agent clotrimazole were evaluated in two double-blind, multicentric trials. Ten investigators reported on a total of 1,361 cases in which a 1% solution or a 1% cream formulation was compared with its respective vehicle. Clotrimazole was therapeutically effective, as confirmed by mycological cure (negative microscopy and culture) and clinical improvement, in tinea pedis, tinea cruris, tinea corporis, pityriasis versicolor, and cutaneous candidasis. Furthermore, species identification established the efficacy of clotrimazole against Trichophyton rubrum, T mentagrophytes, Epidermophyton floccosum, Microsporum canis, Malassezia furfur (Pityrosporum orbiculare), and Candida albicans. Safety was demonstrated by the low incidence of possibly drug-related adverse experiences, namely, 19 (2.7%) of 699 patients who were treated with clotrimazole, of whom four (0.6%) discontinued treatment.

Candida↗
PubMed1977

Antifungal agents used for deep-seated mycotic infections.

The main emphasis in this paper is on the broad-spectrum antifungal agent amphotericin B and the narrow-spectrum agent flucytosine. Amphotericin B remains the cornerstone of antifungal therapy. For the treatment of cryptococcal meningitis, the current recommendation is for the combined use of amphotericin B and flucytosine. 2-Hydrostilbamidine is used only in indolent cases of blastomycosis; this condition is usually treated with amphotericin B. A number of newer agents and combinations of drugs also warrant mention, but clinical experience is limited and these agents or combinations have not been approved for clinical use. Not all patients from whom fungal agents are isolated require treatment and the extent of the fungal infection should be determined when possible for evaluation of the need for treatment.

Amphotericin B↗
PubMed1979

Antifungal agents.

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Antifungal Agents↗
PubMed1978

Target substances of some antifungal agents in the cell membrane.

Copiamycin, an antifungal antibiotic, exhibits antimicrobial activity against a few bacteria in addition to a wide variety of fungi. The methanol extract of Sarcina lutea, one of the most susceptible bacteria, was found to reverse the antimicrobial activity of copiamycin. The reversing activity was associated with the phospholipid fraction of the bacteria. The S. lutea phospholipids also reversed the activities of azalomycin F and miconazole, but not that of clotrimazole. The effects of authentic phospholipids and fatty acids were also investigated. As the antimicrobial activities of copiamycin and azalomycin F were most strongly reversed in the same manner by phospholipids with unsaturated fatty acids and basic hydrophilic groups, the sites on the cell membrane sensitive to both antibiotics are assumed to be identical. On the other hand, the activity of miconazole was affected by different phospholipids from those which affected these two antifungal antibiotics, and the activity of clotrimazole was not affected by any of the phospholipids and fatty acids. It was postulated that the sites on the cell membrane sensitive to miconazole and clotrimazole are different from those sensitive to copiamycin and azalomycin F.

Antifungal Agents↗
PubMed1979

[A contribution to the stereospecific synthesis of antifungal imidazolyloxime-ethers/Oxiconazole nitrate (Sgd 301-76), a new broadspectrum antifungal agent (author's transl)].

A stereospecific synthesis of antifungal imidazolyloxime-ether derivatives is reported. The compound Sgd 301-76 (oxiconazole nitrate) = (Z)-1-(2,4-dichlorophenyl)-2-(1H-imidazol-1-yl)-O-(2,4-dichlorobenzyl)-ethanoneoxime-nitrate was selected for clinical trials. The (E)- and (Z)-assignments, respectively, were made on the basis of 1-H-NMR-spectral data.

Antifungal Agents↗
PubMed2026

A new MRR1 gain-of-function mutation involved in cross-resistance to antifungal agents in the fungal priority pathogen Candida parapsilosis.

OBJECTIVES: Candida parapsilosis is a leading cause of invasive candidiasis globally, with rising reports of fluconazole resistance threatening its clinical management. Among the mechanisms involved, gain-of-function mutations in the MRR1 gene have emerged as key drivers of antifungal resistance. We aimed to investigate a novel amino acid substitution (G982E) in the Mrr1 zinc cluster transcription factor, identified in a fluconazole-resistant C. parapsilosis isolate from a patient exposed to fluconazole. METHODS: Using CRISPR-Cas9 genome editing, we introduced the G982E variant into two fluconazole-susceptible C. parapsilosis genetic backgrounds. The antifungal susceptibility of the engineered mutants was assessed in vitro against a broad panel of systemic antifungal agents. A Galleria mellonella infection model was also used to evaluate the impact of the G982E variant on antifungal treatment efficacy and virulence in vivo. RESULTS: Acquisition of the G982E substitution dramatically altered the antifungal susceptibility profile, particularly for fluconazole for which the MIC increased to >256 µg/mL. However, the magnitude of the MIC increase varied by azole, with the greatest increase seen for fluconazole (>9-10-fold), followed by voriconazole (5-fold), isavuconazole (3-fold), but also flucytosine (1.5-fold). In contrast, susceptibility to posaconazole remained largely unchanged. In vivo, this new variant conferred fluconazole treatment failure but was associated with a significant reduction in virulence. CONCLUSIONS: The G982E is a novel Mrr1 gain-of-function mutation driving high-level fluconazole resistance in C. parapsilosis. These findings reinforce the central role of Mrr1 in antifungal resistance, underscore the functional diversity of its mutational landscape, with potential implications for fungal fitness and transcriptional regulation.

Candida parapsilosis↗
PubMed1978

Antifungal agents.

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Amphotericin B↗
PubMed1978

Antifungal agents.

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Antifungal Agents↗