ChemInform Abstract: SYNTHESIS AND ANTIMYCOTIC ACTIVITY OF α‐ARYL‐β, N‐IMIDAZOLYLALKYL BENZYL ETHERS

Tajana, A; Cappelletti, R; Leonardi, Amedeo; Nardi, D; Veronese, M.

doi:10.1002/chin.198217187

Cited by 3 publications

(3 citation statements)

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“…Three antifungal preparations were used: bifonazole I%, miconazole 2% and fenticonazoe 2% (2,3,4,5,6) and were applied only once 24,48,72 or 96 h prior to the infection of the skin prepared as described above. We used a group without treatments as control.…”

Section: Drugs and Treatmentmentioning

confidence: 99%

Evaluation of the Skin Retention Time of Imidazole Derivative/Die Bewertung der Verweildauer von Imidazolderivaten in der Haut

Veronese

Bertoncini

Preti

1987

Mycoses

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Summary: The evaluation of prophylactic antifungal effect expressed as drug retention time, or as time required for the onset of an experimental mycotic infection in pre‐treated guinea‐pigs, has shown some imidazolederivatives capability to exert this activity even 48 and 72 hours after a single application. The long‐term intracutaneous activity and powerful fungicidal activity of one of the tested drug, fenticonazole, suggest that a single daily administration can be adequate for the treatment of human dermatophytosis. Zusammenfassung: Studien zur Bewertung der prophylaktischen, antimyzetischen Wirkung, ausgedrückt als Verweildauer des Antimykotikums oder als die zum Angehen einer experimentellen Infektion in vorbehandelten Meerschweinchen benötigte Zeit, zeigen einen solchen Effekt bei einigen Imidazolderivaten nach 48 und 72 h nach einmaliger Applikation. Die langanhaltende und starke, intrakutane, fungizide Aktivität eines der geprüften Antimykotika, des Fenticonazols, legt nahe, daß eine jeweils einmalige Anwendung pro Tag für die Behandlung einer Dermatophytose ausreichen dürfte.

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Section: Drugs and Treatmentmentioning

confidence: 99%

Evaluation of the Skin Retention Time of Imidazole Derivative/Die Bewertung der Verweildauer von Imidazolderivaten in der Haut

Veronese

Bertoncini

Preti

1987

Mycoses

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“…Fenticonazole [1] is an imidazole derivative synthesized by the Recordati Research Division (Milan, Italy) [2] , [3] , [4] . It possesses a broad spectrum of antimycotic activity against superficial mycoses (Mycosporum, Tricophyton, and Epidermophyton) [5], as well as deep mycose (candidiasis, trichomoniasis, mixed infection and bacterial vaginosis) [6] , [7] .…”

Section: Introductionmentioning

confidence: 99%

Determination of fenticonazole in human plasma by HPLC–MS/MS and its application to pharmacokinetic studies

Mao

Wang²,

et al. 2017

Journal of Pharmaceutical Analysis

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Two simple and sensitive high performance liquid chromatography–tandem mass spectrometry (HPLC–MS/MS) methods were developed and validated for the determination of fenticonazole in human plasma after percutaneous and intravaginal administration. Mifepristone was used as an internal standard (IS), and simple protein precipitation by acetonitrile containing 2% acetic acid was utilized for extracting the analytes from the plasma samples. Chromatographic separation was performed on a Kinetex XB-C18 column. The quantitation was performed by a mass spectrometer equipped with an electrospray ionization source in multiple reactions monitoring (MRM) positive ion mode using precursor-to-product ion transitions of m/z 455.2–199.1 for fenticonazole and m/z 430.2–372.3 for mifepristone. The validated linear ranges were 5–1000 pg/mL and 0.1–20 ng/mL fenticonazole in plasma for the methods A and B, respectively. For the two methods, the accuracy data ranged from 85% to 115%, the intra- and inter-batch precision data were less than 15%, the recovery data were more than 90%, and no matrix interference was observed. The methods A and B were successfully validated and applied to the pharmacokinetic studies of fenticonazole gel in Chinese healthy volunteers after percutaneous and intravaginal administration, respectively.

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“…Fenticonazole, an imidazole derivative, is apotent broad-spectrum antimycotic with bactericidal activity in vitro as in vivo, against gram-positive bacteria. In preclinical trials it was found to be very active and safe (1)(2)(3)(4)(5)(6)(7)(8)(9). mykosen 29, No.…”

Section: Introductionmentioning

confidence: 99%

A Double Blind Evaluation of Fenticonazole Cream 2% and Clotrimazole Cream 1% in Dermatomycoses/Doppelblindstudie mit Fenticonazol‐Creme 2%ig und Clotrimazol‐Creme 1%ig bei Dermatomykosen

Finzi

Fioroni

Preti

et al. 1986

Mycoses

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Summary: 21 patients suffering from dermatomycoses were randomly assigned either to 2% fenticonazole cream or 1% clotrimazole cream. The study was performed under double‐blind conditions and on patients, with symmetrical or clinically comparable lesions. Patients were evaluated, clinically, microscopically and by culture before entering the study and then at weekly intervals for four weeks. The cream was applied twice daily. Eighteen lesions from the 21 treated with fenticonazole 2% cream and 13 lesions out of 21 treated with clotrimazole 1% cream were definitely cured. The differences between the two treatments were statistically significant in favour of fenticonazole in the third week of treatment (p < 0.05 ‐ chi square test). Zusammenfassung: 21 Patienten mit Dermatomykosen, die symmetrisch lokalisiert und klinisch vergleichbar waren, wurden in einer Doppelblindstudie seitenvergleichend mit 2% Fenticonazol‐Creme und 1% Clotrimazol‐Creme behandelt. Klinische, mikroskopische und kulturelle Untersuchungen wurden vor Beginn der Behandlung und dann in wöchentlichen Intervallen über 4 Wochen durchgeführt. Die Creme wurde zweimal täglich aufgetragen. Bei 18 von 21 mit Fenticonazol 2%‐Creme behandelten Fälle und bei 13 von 21 mit Clotrimazol 1%‐Creme behandelten wurde vollständige Abheilung erreicht. In der dritten Behandlungswoche envies sich das günstigere Behandlungsergebnis mit Fenticonazol als statistisch signifikant (p < 0,05 — chi Quadrattest).

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ChemInform Abstract: SYNTHESIS AND ANTIMYCOTIC ACTIVITY OF α‐ARYL‐β, N‐IMIDAZOLYLALKYL BENZYL ETHERS

Abstract: Die auf dem imFOrmeISChema angegebenen Weg hergestellten Benzylether (III) werden auf antimykotische und antimikrobielle Wirkung getestet.

Cited by 3 publications

References 0 publications

Evaluation of the Skin Retention Time of Imidazole Derivative/Die Bewertung der Verweildauer von Imidazolderivaten in der Haut

Evaluation of the Skin Retention Time of Imidazole Derivative/Die Bewertung der Verweildauer von Imidazolderivaten in der Haut

Determination of fenticonazole in human plasma by HPLC–MS/MS and its application to pharmacokinetic studies

A Double Blind Evaluation of Fenticonazole Cream 2% and Clotrimazole Cream 1% in Dermatomycoses/Doppelblindstudie mit Fenticonazol‐Creme 2%ig und Clotrimazol‐Creme 1%ig bei Dermatomykosen

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