As part of our project devoted to the search for antifungal agents, which act via a selective mode of action, we synthesized a series of new 4-aryl- or 4-alkyl-N-arylamine-1-butenes and transformed some of them into 2...
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As part of our project devoted to the search for antifungal agents, which act via a selective mode of action, we synthesized a series of new 4-aryl- or 4-alkyl-N-arylamine-1-butenes and transformed some of them into 2-substituted 4-methyl-tetrahydroquinolines and quinolines by using a novel three-step synthesis. Results obtained in agar dilution assays have shown that 4-aryl homoallylamines not possessing halogen in their structures, tetrahydroquinolines and quinolines, display a range of antifungal properties in particular against Epidermophyton floccosum and Microsporum canis. Regarding the mode of action, all active compounds showed in vitro inhibitory activities against beta(1-3) glucan-synthase and mainly against chitin-synthase. These enzymes catalyze the synthesis of beta(1-3) glucan and chitin, respectively, major polymers of the fungal cell wall. Since fungal but not mammalian cells are encased in a cell wall, its inhibition may represent a useful mode of action for these antifungal compounds. (C) 2000 Elsevier Science Ltd. All rights reserved.
Benzyl, furfuryl, tetrahydronaphthyl, alpha-picolyl, and alpha-homopicolyl derivatives of 2-thiotetrahydro-1,3,5-thiadiazines were studied and found to be more active than beta-picolyl, and pyridyl analogs on dermatop...
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Benzyl, furfuryl, tetrahydronaphthyl, alpha-picolyl, and alpha-homopicolyl derivatives of 2-thiotetrahydro-1,3,5-thiadiazines were studied and found to be more active than beta-picolyl, and pyridyl analogs on dermatophytes, including the more resistant Microsporum canis.
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