Mikrobiol. Z. 2019; 81(2):73-83. Ukrainian.
Antifungal Activity of Arylaliphatic Aminopropanol Derivative 1-[4-(1,1,3,3-Tetramethylbutyl)phenoxy]-
Institute of Pharmacology and Toxicology, NAMS of Ukraine
14 A. Tsedika Str., Kyiv, 03057, Ukraine
Aim. The purpose of the work was to investigate the antifungal activity of the arylaliphatic aminopropanol derivative 1-[4-(1,1,3,3-tetramethylbutyl)phenoxy]-3-(N-benzyl-4-methylpiperidinium)-2-propanol chloride (KVM-204) against yeasts, filamentous fungi and dermatophytes. Methods. The susceptibility of the fungi to the compound KVM-204 was determined by two-fold broth dilution method and evaluated by the means of the minimum inhibitory concentration (MIC). The determination of cytomorphological features of filamentous fungi under the action of compound was carried out by light microscopy. The effect of KVM-204 on the germ-tubes formation was investigated against fungi the genus Candida by the method of Larone. Results. The compound KVM-204 possess a wide spectrum of anti-candida activity, the inhibitory effect of compound is close to fluconazole and itraconazole (except Candida parapsilosis). It has been established that the arylaliphatic aminopropanol derivative possess antifungal activity against Trichophyton mentagrophytes var. gypseum, according to the MIC, compound is not inferior to fluconazole. Exposure of arylaliphatic aminopropanol derivative KVM-204 at 1.0 MIC on filamentous fungi causes significant cytomorphological alterations in the cell wall of the microorganisms. Compound KVM-204 at 1.0 MIC and 5.0 MIC inhibits the formation of germ-tubes by Candida albicans, the action of the compound is comparable to that of amphotericin B. Conclusions. Studies on antifungal activity have shown that the compound KVM-204 possess a pronounced anticandida effect. The KVM-204 also alters the morphology of filamentous fungi and inhibits the formation of germ-tubes by Candida spp., influencing the pathogenicity of yeasts.
Keywords: antifungal activity, arylaliphatic aminopropanol derivative, dermatophytes, fungi the genus Candida, filamentous fungi.
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