Antifungal agents

D’Arcy, P. F.; Scott, Eileen

doi:10.1007/978-3-0348-7102-0_3

Cited by 9 publications

(10 citation statements)

References 346 publications

Supporting

Mentioning

Contrasting

Unclassified

Order By: Relevance

“…However, the MICs of only 8 of 77 isolates exceeded 100 ,ug/ml. Thus the activity spectrum of naftifine differs from that of tolnaftate, which is completely inactive against yeasts of the genus Candida (2,4,5).…”

Section: Resultsmentioning

confidence: 99%

“…The current therapy of dermatomycoses depends mainly on antifungal agents belonging to four different chemical groups: the imidazoles, thiocarbamates, and antibiotics such as the polyenes or griseofulvin (2,4). This report deals with the antifungal properties of naftifine, which is an allylamine derivative and represents a new chemical group of antifungal compounds.…”

mentioning

confidence: 99%

See 1 more Smart Citation

In vitro activity of naftifine, a new antifungal agent

Georgopoulos¹,

Petrányi²,

Mieth³

et al. 1981

Antimicrob Agents Chemother

102

View full text Add to dashboard Cite

Naftifine exhibits an interesting in vitro spectrum of activity against dermatophytes (38 strains; minimal inhibitory concentration [MIC] range, 0.1 to 0.2 ,ug/ ml), aspergilli (6 strains; MIC range, 0.8 to 12.5 jig/ml), Sporothrix schenckii (2 strains; MICs, 0.8 and 1.5 ,ug/ml), and yeasts of the genus Candida (77 strains; MIC range, 1.5 to >100 ,ug/ml). Its degree of efficacy is unaffected by the organism density in the test medium, and it is primarily fungicidal against dermatophytes as well as yeasts. Its in vitro efficacy is pH dependent and rises with increasing pH values.

show abstract

Section: Resultsmentioning

confidence: 99%

mentioning

confidence: 99%

In vitro activity of naftifine, a new antifungal agent

Georgopoulos¹,

Petrányi²,

Mieth³

et al. 1981

Antimicrob Agents Chemother

102

View full text Add to dashboard Cite

show abstract

“…The discovery and refinement of azole drugs has relied entirely on whole-cell testing (2). Structure based approaches to designing more efficacious azoles have been stymied by the fact that the drug target site, CYP51, is an integral membrane protein and has proven difficult to purify and crystallize.…”

Section: Discussionmentioning

confidence: 99%

Three-Dimensional Models of Wild-Type and Mutated Forms of Cytochrome P450 14α-Sterol Demethylases from Aspergillus fumigatus and Candida albicans Provide Insights into Posaconazole Binding

Xiao¹,

Madison²,

Chau³

et al. 2004

Antimicrob Agents Chemother

259

215

View full text Add to dashboard Cite

The cytochrome P450 sterol 14␣-demethylase enzyme (CYP51) is the target of azole antifungals. Azoles block ergosterol synthesis, and thereby fungal growth, by binding in the active-site cavity of the enzyme and ligating the iron atom of the heme cofactor through a nitrogen atom of the azole. Mutations in and around the CYP51 active site have resulted in azole resistance. In this work, homology models of the CYP51 enzymes from Aspergillus fumigatus and Candida albicans were constructed based on the X-ray crystal structure of CYP51 from Mycobacterium tuberculosis. Using these models, binding modes for voriconazole (VOR), fluconazole (FLZ), itraconazole (ITZ), and posaconazole (POS) were predicted from docking calculations. Previous work had demonstrated that mutations in the vicinity of the heme cofactor had a greater impact on the binding of FLZ and VOR than on the binding of POS and ITZ. Our modeling data suggest that the long side chains of POS and ITZ occupy a specific channel within CYP51 and that this additional interaction, which is not available to VOR and FLZ, serves to stabilize the binding of these azoles to the mutated CYP51 proteins. The model also predicts that mutations that were previously shown to specifically impact POS susceptibility in A. fumigatus and C. albicans act by interfering with the binding of the long side chain.

show abstract

“…However, the development of effective antifungal agents has been disappointingly slow. Thrush, an oral manifestation of Candida albicans infection, was recorded in 1665 as a fatal disease (63). In 1835, Bassi de Lodi determined that the causative agent of muscardine, i.e., silkworm disease, was a fungus that multiplied within and on the insect.…”

Section: Introductionmentioning

confidence: 99%

Overview of medically important antifungal azole derivatives

1988

View full text Add to dashboard Cite

Fungal infections are a major burden to the health and welfare of modern humans. They range from simply cosmetic, non-life-threatening skin infections to severe, systemic infections that may lead to significant debilitation or death. The selection of chemotherapeutic agents useful for the treatment of fungal infections is small. In this overview, a major chemical group with antifungal activity, the azole derivatives, is examined. Included are historical and state of the art information on the in vitro activity, experimental in vivo activity, mode of action, pharmacokinetics, clinical studies, and uses and adverse reactions of imidazoles currently marketed (clotrimazole, miconazole, econazole, ketoconazole, bifonazole, butoconazole, croconazole, fenticonazole, isoconazole, oxiconazole, sulconazole, and tioconazole) and under development (aliconazole and omoconazole), as well as triazoles currently marketed (terconazole) and under development (fluconazole, itraconazole, vibunazole, alteconazole, and ICI 195,739).

show abstract

Antifungal agents

Cited by 9 publications

References 346 publications

In vitro activity of naftifine, a new antifungal agent

In vitro activity of naftifine, a new antifungal agent

Three-Dimensional Models of Wild-Type and Mutated Forms of Cytochrome P450 14α-Sterol Demethylases from Aspergillus fumigatus and Candida albicans Provide Insights into Posaconazole Binding

Overview of medically important antifungal azole derivatives

Contact Info

Product

Resources

About