ChemInform Abstract: NEW α‐ARYL‐β, N‐IMIDAZOLYLETHYL BENZYL AND NAPHTHYLMETHYL ETHERS WITH ANTIMYCOTIC AND ANTIBACTERIAL ACTIVITY

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

doi:10.1002/chin.198217186

Cited by 4 publications

(4 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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“…To the best of our knowledge, before our first study on this topic was published, no mention was still made in the literature of compounds owning both antifungal and antimycobacterial activities, with the only exception of a few azole derivatives [9]. On the other hand, since all of compounds previously mentioned, known to be active as antibacterials, revealed also very active against mycobacteria (for example fluoroquinolones and oxazolidinones [10][11][12]) the two activities have been correlated each other.…”

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confidence: 95%

BM 212 and its Derivatives as a New Class of Antimycobacterial Active Agents

Biava

2002

CMC

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During our investigation in pyrrole antibacterial area we have identified a subclass with a good potent in vitro activity against mycobacteria and fungi. We have individuated the salient structural feature and BM 212 as lead for the class. SAR studies allowed us to synthesize several analogue derivatives. Some of them revealed more active than BM 212 against mycobacteria, but they lost antifungal activity. In particular the Protection Index (PI) was very interesting for some derivatives, comparable to that of reference compounds, Isoniazid (INH), Streptomycin (SM) and Rifampin (RF). Many of the synthesized compounds revealed active against intracellular mycobacteria and they showed to be inhibitory to drug-resistant mycobacteria of clinical origin. On the base of microbiological results we have hypothesized a pharmacophore model that was also optimized. The rational design, and the evaluation of the in vitro activity against mycobacteria are described.

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ChemInform Abstract: NEW α‐ARYL‐β, N‐IMIDAZOLYLETHYL BENZYL AND NAPHTHYLMETHYL ETHERS WITH ANTIMYCOTIC AND ANTIBACTERIAL ACTIVITY

Abstract: Die durch Umsetzung von Imidazolylethanolen (I) mit Benzylhalogeniden (II) erhaltenen Ether (III) werden auf antimykotische und antimikrobielle Aktivität geprüft.

Cited by 4 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

BM 212 and its Derivatives as a New Class of Antimycobacterial Active Agents

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