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Allylamine Antifungal Drugs

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Current Topics in Medical Mycology

Part of the book series: Current Topics in Medical Mycology ((CT MYCOLOGY,volume 4))

Abstract

The allylammes constitute a recently developed class of synthetic antimycotics characterized functionally by their action as squalene epoxidase inhibitors.1 Figure 6–1 shows the structures of three representative allylamines. Naftifine, the first of these compounds to be discovered, was first synthesized in 1974,2 and its antifungal properties were identified during routine screening. The potent antifungal activity of naftifine in vitro3 and in vivo4 led to its clinical development, and this drug has been marketed since 1985 as a topical antimycotic. Naftifine provided the basis for an extensive program of chemical derivatization5–8 aimed at improving the antimycotic efficacy, especially with regard to oral administration. This goal was achieved in the form of terbinafine (SF 86–327), 1,6–13 the efficacy of which has now been confirmed in numerous clinical studies involving both topical and oral application. Parallel to this development, detailed investigations were carried out concerning the mechanism of action of the allylamines,14–26 including much basic research on the biochemistry of ergosterol biosynthesis in pathogenic fungi.

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Authors
  1. Neil S. Ryder
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  2. Hubert Mieth
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Editor information

Editors and Affiliations

  1. Life Sciences, Janssen Research Foundation, B-2340, Beerse, Belgium

    Marcel Borgers Ph.D.

  2. Department of Dermatology, Guy’s Hospital, SE1 9RT, London Bridge, London, UK

    Roderick Hay M.D.

  3. Health Science Center at San Antonio, University of Texas, 78284-7750, San Antonio, Texas, USA

    Michael G. Rinaldi Ph.D.

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© 1992 Springer-Verlag New York Inc.

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Ryder, N.S., Mieth, H. (1992). Allylamine Antifungal Drugs. In: Borgers, M., Hay, R., Rinaldi, M.G. (eds) Current Topics in Medical Mycology. Current Topics in Medical Mycology, vol 4. Springer, New York, NY. https://doi.org/10.1007/978-1-4612-2762-5_6

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  • DOI: https://doi.org/10.1007/978-1-4612-2762-5_6

  • Publisher Name: Springer, New York, NY

  • Print ISBN: 978-1-4612-7657-9

  • Online ISBN: 978-1-4612-2762-5

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