Optically Active Antifungal Azoles. XII. Synthesis and Antifungal Activity of the Water-Soluble Prodrugs of l-[(lR, 2R)-2-(2, 4-Difluorophenyl)-2-hydroxy-l-methyl-3-(1H-1, 2, 4-triazol-1-yl)propyl]3-[4-(lH-1-tetrazolyl)phenyl]-2-imidazolidinone

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概要

• 論文の詳細を見る

• 1-[(1R, 2R)-2-(2, 4-Difluorophenyl)-2-hydroxy-1-methyl-3-(lH-1, 2, 4-triazol-1-yl)propyl]-3-[4-(1H-1-tetrazolyl)phenyl]-2-imidazolidinone (1: TAK-456) was selected as a candidate for clinical trials, but since its watersolubility was insufficient for an injectable formulation, the quaternary triazolium salts 2 were designed as watersoluble prodrugs. Among the prodrugs prepared, 4-acetoxymethyl-1-[(2R, 3R)-2-(2, 4-difluorophenyl)-2-hydroxy-3-[2-oxo-3-[4-(1H-1-terazolyl)phenyl]-1-imidazolidinyl]butyl]-1H-1, 2, 4-triazolium chloride (2a: TAK-457) was selected as an injectable candidate for clinical trials based on the results of evaluations on solubility, stability, hemolytic effect and in vivo antifungal activities.

• 公益社団法人日本薬学会の論文
• 2001-09-01

著者

• Yamada Makiko

  San-ei Gen F.f.i. Inc.

• Itoh K

  Medicinal Chemistiy Research Laboratories I Pharmaceutical Research Division Takeda Chemical Industr

• Itoh K

  Pharmaceutical Research Laboratories Iii Pharmaceutical Research Division Takeda Chemical Industries

• Yamada M

  Pharmaceutical Research Division Takeda Pharmaceutical Company Limited

• Yoshida M

  Tohoku Univ. Sendai Jpn

• Ichikawa Takashi

  Pharmaceutical Research Division Takeda Pharmaceutical Company Limited

• ICHIKAWA Takashi

  Medicinal Chemistry Research Laboratories I, Pharmaceutical Research Division, Takeda Chemical Indus

• YAMADA Masami

  Medicinal Chemistry Research Laboratories II, Pharmaceutical Research Division, Takeda Chemical Indu

• YAMAGUCHI Masashi

  Drug Analysis & Pharmacokinetic Research Laboratories, Pharmaceutical Research Division, Takeda Chem

• KITAZAKI Tomoyuki

  Medicinal Chemistry Research Laboratories II, Pharmaceutical Research Division, Takeda Chemical Indu

• MATSUSHITA Yoshihiro

  Medicinal Chemistry Research Laboratories I, Pharmaceutical Research Division, Takeda Chemical Indus

• ITOH Katsumi

  Medicinal Chemistry Research Laboratories I, Pharmaceutical Research Division, Takeda Chemical Indus

• HAYASHI Ryogo

  Pharmacology Research Laboratories II, Pharmaceutical Research Division, Takeda Chemical Industries,

• KIYOTA Yutaka

  Drug Analysis & Pharmacokinetics Research Laboratories, Pharmaceutical Research Division, Takeda Che

• OKONOGI Kenji

  Research Management Department, Pharmaceutical Research Division, Takeda Chemical Industries, Ltd.

• Kiyota Yutaka

  Drug Analysis & Pharmacokinetics Research Laboratories Pharmaceutical Research Division Takeda C

• Itoh Katsumi

  Medicinal Chemistiy Research Laboratories I Pharmaceutical Research Division Takeda Chemical Industr

• Ichikawa T

  Pharmaceutical Research Division Takeda Pharmaceutical Company Limited

• Itoh K

  Graduate School Of Pharmaceutical Sciences Chiba University:nisshin Seifun Group Inc.

• Itoh Kinuyo

  Department Of Materials Chemistry & Frontier Research Center Graduate School Of Engineering. Osa

• Itoh Kunihiko

  Dept. Pharmaceutical Sciences Akita University

• Hayashi R

  Pharmacology Research Laboratories Ii Pharmaceutical Research Division Takeda Chemical Industries Lt

• Okonogi K

  Pharmacology Research Laboratories I Pharmaceutical Research Division Takeda Chemical Industries Ltd

• Kitazaki T

  Pharmaceutical Research Division Takeda Pharmaceutical Company Limited

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