Structure-Activity Relationships of a New Antifungal Imidazole, AFK-108,and Related Compounds

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概要

• 論文の詳細を見る

• Fungicidal activity of widely used imidazole antifungal drugs in topical applications is not so strong in spite of their potent fungistatic activities against dermatophytes and pathogenic yeasts. In order to improve fungicidal activity of imicazole antifungal agents, a series of novel imidazole derivatives having a hydrophobic substituent derived from isoprenoid were synthesized. The efficacy of these compounds was evaluated with respect to direct cell-membrane damaging activity, ergosterol biosynthesis inhibition, minimum growth-inhibitory concentration (MIC) and therapeutic effect for experimental dermatophytosis of guinea pigs. Among the newly synthesized compounds, the geranyl derivative named AFK-108 (2a) showed the highest in vivo fungicidal activity with both cell membrane damaging activity and ergosterol biosynthesis inhibition in vitro.

• 公益社団法人日本薬学会の論文
• 2000-01-01

著者

• YOSHIDA Yuzo

  School of Pharmaceutical Sciences, Mukogawa Women's University

• Yoshida Yuzo

  School O Pharmaceutical Sciences Mukogawa Women's University

• Ishida K

  Biological Science Laboratories Kao Co. Ltd.

• HORI Kimihiko

  Biological Science Laboratories, KAO Co., Ltd.,

• SAKAGUCHI Akira

  Biological Science Laboratories, KAO Co., Ltd.,

• KUDOH Michinari

  Biological Science Laboratories, KAO Co., Ltd.,

• ISHIDA Koichi

  Biological Science Laboratories, KAO Co., Ltd.,

• AOYAMA Yuri

  School of Pharmaceutical Sciences, Mukogawa Women's University

• Aoyama Y

  School Of Pharmaceutical Sciences Mukogawa Women's University:(present Address)department Of Bi

• Hori Kimihiko

  Biological Science Laboratories Kao Co. Ltd.

• KUDOH Michinari

  Teikyo University Institute of Medical Mycology

• Sakaguchi Akira

  Biological Science Laboratories Kao Co. Ltd.

• AOYAMA Yuri

  School of Pharmaceutical Sciences, Mukogawa Women's University:(Present address)Department of Bioengineering, Faculty of Engineering, Soka University

関連論文

• The Construction and Characterization of Self-Sufficient Lanosterol 14-Demethylase Fusion Proteins Consisting of Yeast CYP51 and Its Reductase(Biochemistry)
• Evidence for Recycling of Cytochrome P450 Sterol 14-Demethlase from the cis-Golgi Compartment to the Endoplasmic Reticulum (ER) upon Saturation of the ER-retention Mechanism
• Structure-Activity Relationships of a New Antifungal Imidazole, AFK-108,and Related Compounds
• Effects of Y132H and F145L Substitutions on the Activity, Azole Resistance and Spectral Properties of Candida albicans Sterol 14-Demethylase P450 (CYP51) : A Live Example Showing the Selection of Altered P450 through Interaction with Environmental Compoun
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• Foreword
• The Amino Acid Residues Affecting the Activity and Azole Susceptibility of Rat CYP51 (Sterol 14-Demethylase P450).
• Structural and Evolutionary Studies on Sterol 14-Demethylase P450 (CYP51), the Most Conserved P450 Monooxygenase: I. Structural Analyses of the Gene and Multiple Sizes of mRNA.
• Structural and Evolutionary Studies on Sterol 14-Demethylase P450 (CYP51), the Most Conserved P450 Monooxygenase: II. Evolutionary Analysis of Protein and Gene Structures.

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