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- W2002733668 abstract "<i>Background:</i>In contrast to the increasing numbers of agents for the treatment of invasive fungal infections, discoveries of new antifungal agents with therapeutic value in dermatomycoses are reported only rarely. <i>Methods:</i> Abafungin (chemical abstracts service registry No. 129639-79/8) is the first member of a novel class of synthetic antifungal compounds, the arylguanidines. It was first synthesized at Bayer AG, Leverkusen, Germany, and its antifungal action was discovered during the screening of H<sub>2</sub>-receptor antagonists based on the structure of famotidine. To obtain insight into its mode of action and antifungal activity, various tests were carried out with different fungal pathogensin vitro. <i>Results:</i> Abafungin was found to have potent antifungal activity. Furthermore, mode-of-action studies suggested that abafungin exerts its antifungal activity regardless of whether the pathogens are growing or in a resting state. One target of abafungin was found to be the inhibition of transmethylation at the C-24 position of the sterol side chain, catalyzed by the enzyme sterol-C-24-methyltransferase. A second action of abafungin seems to be a direct effect on the fungal cell membrane.<i>Conclusion:</i> The observed characteristics of abafungin indicate that abafungin might be a promising antifungal agent defining a new class of antimycotics." @default.
- W2002733668 created "2016-06-24" @default.
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- W2002733668 date "2008-01-01" @default.
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- W2002733668 title "Modes of Action of the New Arylguanidine Abafungin beyond Interference with Ergosterol Biosynthesis and in vitro Activity against Medically Important Fungi" @default.
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- W2002733668 doi "https://doi.org/10.1159/000142334" @default.
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