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烯丙胺衍生物的抗皮肤癣菌活性。

Antidermatophytic activity of allylamine derivatives.

作者信息

Venugopal P V, Venugopal T V

机构信息

Institutes of Microbiology, Madurai Medical College, India.

出版信息

Indian J Pathol Microbiol. 1994 Oct;37(4):381-8.

PMID:7868170
Abstract

The allylamine derivatives are a new class of synthetic antifungal agents. The antidermatophytic activity of the two main compounds, naftifine and terbinafine were compared in vitro with those of ketoconazole and itraconazole by agar dilution. Eighty eight clinical isolates of dematophytes comprising of Microsporum canis (50), M. audouinii (5), Trichophyton rubrum (6) T. mentagrophytes (5), T. violaceum (12), T. simii (5), T. verrucosum (1), T. soudanense (1), T. erinacie (1) and Epidermophyton floccosum (2) were tested. Terbinafine was found to be most active, inhibiting 68 of the 88 isolates at a concentration of 0.01 ug ml-1 and all at 0.1 ug ml. (Minimum inhibitory concentration - MIC range < or = 0.0001-0.1 ug ml-1). Naftifine inhibited 84 isolates at a concentration of 0.1 ug ml-1 and all at 0.5 ug ml-1 (MIC range 0.001-0.5 ug ml-1). Itraconazole required 0.1 ug ml-1 for inhibiting 50 isolates and 0.5 ug ml-1 for 85 isolates (MIC range 0.01-1 ug ml-1) whereas ketoconazole inhibited 71 isolates at 1 ug ml-1 and 87 at 2.5 ug ml-1 (MIC range 0.01-5 ug ml-1).

摘要

烯丙胺衍生物是一类新型的合成抗真菌药物。通过琼脂稀释法,在体外比较了两种主要化合物萘替芬和特比萘芬与酮康唑和伊曲康唑对皮肤癣菌的抗真菌活性。测试了88株临床分离的皮肤癣菌,包括犬小孢子菌(50株)、奥杜盎小孢子菌(5株)、红色毛癣菌(6株)、须癣毛癣菌(5株)、紫色毛癣菌(12株)、石膏样毛癣菌(5株)、疣状毛癣菌(1株)、苏丹毛癣菌(1株)、猬毛癣菌(1株)和絮状表皮癣菌(2株)。结果发现特比萘芬活性最强,在浓度为0.01μg/ml时可抑制88株中的68株,在0.1μg/ml时可抑制所有菌株(最低抑菌浓度 - MIC范围≤0.0001 - 0.1μg/ml)。萘替芬在浓度为0.1μg/ml时可抑制84株,在0.5μg/ml时可抑制所有菌株(MIC范围0.001 - 0.5μg/ml)。伊曲康唑抑制50株需要0.1μg/ml,抑制85株需要0.5μg/ml(MIC范围0.01 - 1μg/ml),而酮康唑在1μg/ml时可抑制71株,在2.5μg/ml时可抑制87株(MIC范围0.01 - 5μg/ml)。

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