Correlation between antifungal activity and hydrophobicity of imidazole antifungal agents.
To examine the effects of the affinity of antifungal imidazole agents to cell membranes on the in vitro antifungal activity, the correlation between antifungal activity and hydrophobicity of these drugs was investigated. The capacity factor (k') in HPLC was used as a parameter of hydrophobicity, and the minimum inhibitory concentration (MIC) as a parameter of antifungal activity. Consequently, a significant portion correlation was noted in the case of Candida albicans. However, no obvious correlation was noted for Trichophyton mentagrophytes and Trichophyton rubrum. Therefore, the mechanism of action of imidazole derivatives for Candida albicans was considered to mainly consist in the membrane action.
Hashiguchi
T
T
Tsukuba Research Laboratories, Hisamitsu Pharmaceutical Co., Inc., Japan.
Itoyama
T
T
Kodama
A
A
Uchida
K
K
Yamaguchi
H
H
D000935:Antifungal Agents / Q000737:chemistry / Q000494:pharmacology*; D002462:Cell Membrane / Q000737:chemistry / Q000187:drug effects; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D002851:Chromatography, High Pressure Liquid; D005658:Fungi / Q000187:drug effects*; D007093:Imidazoles / Q000737:chemistry / Q000494:pharmacology*; D008826:Microbial Sensitivity Tests; D012044:Regression Analysis; D013329:Structure-Activity Relationship
D000935:Antifungal Agents; D007093:Imidazoles