Triazole Antifungals. II. : Synthesis and Antifungal Activities of 3-Acyl-4-methyloxazolidine Derivatives

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概要

• 論文の詳細を見る

• Triazole compounds with an oxazolidine ring were designed and synthesized as a potential inhibitor of the fungal cytochrome P_<450> 14α-demethylase. In testing for antifungal activity against a mouse systemic Candida albicans infection, (4R, 5R)-3-acyl-4-methyloxazolidine derivatives 4 exhibited remarkably high efficacy after oral or parenteral dosing. The potent activity of 4 is hypothesized to be a consequence of a structural similarity between 4 and lanosterol, a target molecule of the cytochrome P_<450> 14α-demethylase. Highly stereoselective synthesis of these oxazolidines is also described.

• 社団法人日本薬学会の論文
• 1990-09-25

著者

• 安田 紘

  Biological Research Laboratories Sankyo Co. Ltd.

• 宮岡 武男

  Medicinal Chemistry Research Laboratories Sankyo Co. Ltd.

• 鴻巣 俊之

  Medicinal Chemistry Research Laboratories, Sankyo Co., Ltd.,

• 田島 和

  Medicinal Chemistry Research Laboratories, Sankyo Co., Ltd.,

• 老田 貞夫

  Medicinal Chemistry Research Laboratories, Sankyo Co., Ltd.,

• 武田 憲子

  Medicinal Chemistry Research Laboratories Sankyo Co., Ltd.

• 笠原 真由美

  Biological Research Laboratories, Sankyo Co., Ltd.,

• 武田 憲子

  Medical Chemistry Research Laboratories Sankyo Co. Ltd.

• 田島 和

  Medicinal Chemistry Research Laboratories Sankyo Co. Ltd.

• 老田 貞夫

  Medicinal Chemistry Research Laboratories Sankyo Co. Ltd.

• 鴻巣 俊之

  Medicinal Chemistry Research Laboratories Sankyo Co. Ltd.

• 笠原 真由美

  Biological Research Laboratories Sankyo Co. Ltd.

• 鴻巣 俊之

  Medicinal Chemistry Res. Laboratories Ii Daiichi Sankyo Co. Ltd.

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