The objective of this study was to compare the anti-inflammatory potencies of the imidazole antimycotics, fluconazole, itraconazole, ketoconazole and voriconazole (0.5 and 5 microM) in relation to their molecular structures. Anti-inflammatory activity was determined according to the magnitude of inhibition of production of leukotriene B4 and influx of Ca2+ following activation of the cells with the chemo-attractant platelet-activating factor (200 nM), using enzyme-linked immunosorbent assay and spectrofluorometric procedures, respectively. Treatment of platelet-activating factor-activated neutrophils with the imidazole antimycotics resulted in inhibition of production of leukotriene B4 and attenuation of Ca2+ influx, the order of potency being itraconazole > ketoconazole > fluconazole = voriconazole. These observations demonstrate the requirement for both the diazole/triazole moiety (all four agents), and the substituted phenylpiperazinyl ether side chain (itraconazole and ketoconazole only) for maximal anti-inflammatory activity of this class of pharmacological agents.

中文翻译：

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咪唑类抗真菌药的抗炎活性与分子结构的比较。

这项研究的目的是比较咪唑类抗真菌药，氟康唑，伊曲康唑，酮康唑和伏立康唑（0.5和5 microM）在分子结构方面的抗炎作用。使用酶联免疫吸附测定法和荧光分光光度法，根据用化学吸引剂血小板活化因子（200 nM）活化细胞后，对白三烯B4产生的抑制作用和Ca2 +流入的抑制程度，确定抗炎活性。分别。用咪唑类抗真菌药处理血小板活化因子激活的中性粒细胞可抑制白三烯B4的产生并减弱Ca2 +流入，效力的顺序为伊曲康唑>酮康唑>氟康唑=伏立康唑。