Current and Emerging Azole Antifungal Agents

Sheehan, Daniel J.; Hitchcock, Christopher A.; Sibley, Carol M.

doi:10.1128/cmr.12.1.40

Cited by 979 publications

(518 citation statements)

References 214 publications

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“…The fi rst azole drugs developed were the imidazoles such as miconazole (MCZ) and ketoconazole (KTZ). 43 These drugs are relatively insoluble. Imidazoles were followed by triazoles, such as FLC, which have increased water solubility and improved pharmacokinetic properties.…”

Section: Current Treatments For Oral Fungal Infectionsmentioning

confidence: 99%

Antifungal drug resistance of oral fungi

2010

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Fungi comprise a minor component of the oral microbiota but give rise to oral disease in a significant proportion of the population. The most common form of oral fungal disease is oral candidiasis, which has a number of presentations. The mainstay for the treatment of oral candidiasis is the use of polyenes, such as nystatin and amphotericin B, and azoles including miconazole, fluconazole, and itraconazole. Resistance of fungi to polyenes is rare, but some Candida species, such as Candida glabrata and C. krusei, are innately less susceptible to azoles, and C. albicans can acquire azole resistance. The main mechanism of high-level fungal azole resistance, measured in vitro, is energy-dependent drug efflux. Most fungi in the oral cavity, however, are present in multispecies biofilms that typically demonstrate an antifungal resistance phenotype. This resistance is the result of multiple factors including the expression of efflux pumps in the fungal cell membrane, biofilm matrix permeability, and a stress response in the fungal cell. Removal of dental biofilms, or treatments to prevent biofilm development in combination with antifungal drugs, may enable better treatment and prevention of oral fungal disease.

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Section: Current Treatments For Oral Fungal Infectionsmentioning

confidence: 99%

Antifungal drug resistance of oral fungi

2010

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“…Azoles are the most widely used antifungal drugs for systemic fungal infections (Genin et al, 2000;Sheehan et al, 1999;Sheng et al, 2006). The first antifungal azoles were imidazoles such as econazole, miconazole, isoconazole, and ketoconazole (Fig.…”

Section: Introductionmentioning

confidence: 99%

Click chemistry inspired synthesis of piperazine-triazole derivatives and evaluation of their antimicrobial activities

et al. 2015

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A series of novel piperazine-1,2,3-triazole derivatives, which entailed the bioisosteric replacement of the imidazole moiety and hybridization of two drug scaffolds was prepared by employing the regioselective copper (I)-catalysed azide-alkyne 1,3-dipolar cycloaddition reaction. The synthesized compounds were evaluated for antibacterial activities against Gram-negative (E. Coli and P. Putida), Gram-positive S. Aureus bacteria and fungicidal activities against F. oxysporum, F. gramillarium and F. monalliforme fungi. Compound 7ac 0 exhibited moderate but promising antibacterial activity against Gram-negative bacteria and fungicidal activity against F. oxysporum and F. gramillarium.

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“…Especially, azole antifungal agents (e.g., bifonazole) 1 and allylamine antifungals (e.g., terbinafine) 2 are very widely used as therapeutic agents for dermatophyte infections. The efficacy of antifungal agents is primarily evaluated by in vitro antifungal susceptibility tests.…”

Section: Introductionmentioning

confidence: 99%