Allylamine derivatives: new class of synthetic antifungal agents inhibiting fungal squalene epoxidase.
نویسندگان
چکیده
A new class of synthetic antifungal agents, the allylamines , has been developed by modification of naftifine , a topical antimycotic. SF 86-327, the most effective of these compounds so far, is highly active in vitro against a wide range of fungi and exceeds clinical standards in the oral and topical treatment of guinea pig dermatophytoses. SF 86-327 is a powerful specific inhibitor of fungal squalene epoxidase, a key enzyme in sterol biosynthesis.
منابع مشابه
Inhibition of squalene epoxidase and sterol side-chain methylation by allylamines.
Irrtrotliictiori The allylamines arc a recently developed class o f synthetic antifungal agents 1 1 1 with clinical applications against pathogenic fungi. The topical antimycotic na temically active compound terbinafine inhibit a wide range of fungi. with a strictly fungicidal action in most cases [2, 31. A large number of structurally related allylamines have been synthesized; the chemistry an...
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Fig. 1. StcJrol hiosynthesis squalene to lanosterol. This enzyme has been shown to hc essential f o r fungi; Sacchurornyces cerevisiue mutants lacking this key enzyme in fact require exogenous ergosterol supplementation for growth 121. Even if these early steps in sterol biosynthesis are common to mammals and fungi, the example of the allylamines. which act on squalene epoxidase 131. shows that...
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onychomycosis. Clin Exp Dermatol 1987;12:175-7. 8 Petranyi G, Ryder NS,-Stutz A. Allylamine derivatives: new class of synthetic antifungal agents inhibiting fungal squalene epoxidase. Science 1984;224: 1239-41. 9 Stutz A. Synthesis and structure-activity correlations within allylamine antimycotics. Ann N Y Acad Sci 1988;544:46-62. 10 Van de Bossche H, Willemsens G, Cools W, Lauwers WFJ, Lejeune...
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Candida albicans, the most important opportunistic fungal pathogen, is able to generate remarkable amounts of reactive oxygen species (ROS). Since ROS are highly cytotoxic, this mechanism may contribute to the pathogenicity of this yeast, including its invasiveness and the inflammatory response of the host. Terbinafine, a synthetic antifungal agent of the allylamine class, inhibits ergosterol b...
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ورودعنوان ژورنال:
- Science
دوره 224 4654 شماره
صفحات -
تاریخ انتشار 1984