Art

J-GLOBAL ID：200902195138556740   Reference number：01A0863352

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

光学活性抗真菌性アゾール類 XII 1-[(1R,2R)-2-(2,4-ジフルオロフェニル)-2-ヒドロキシ-1-メチル-3-(1H-1,2,4-トリアゾール-1-イル)プロピル]-3-[4-(1H-1-テトラゾリル)フェニル]-2-イミダゾリジノンの水溶性プロドラッグの合成及び抗真菌活性

Author (9)： ICHIKAWA T (Takeda Chemical Ind. Ltd., Osaka, JPN) ,  KITAZAKI T (Takeda Chemical Ind. Ltd., Osaka, JPN) ,  MATSUSHITA Y (Takeda Chemical Ind. Ltd., Osaka, JPN) ,  YAMADA M (Takeda Chemical Ind. Ltd., Osaka, JPN) ,  HAYASHI R (Takeda Chemical Ind. Ltd., Osaka, JPN) ,  YAMAGUCHI M (Takeda Chemical Ind. Ltd., Osaka, JPN) ,  KIYOTA Y (Takeda Chemical Ind. Ltd., Osaka, JPN) ,  OKONOGI K (Takeda Chemical Ind. Ltd., Osaka, JPN) ,  ITOH K (Takeda Chemical Ind. Ltd., Osaka, JPN)
Material： Chemical and Pharmaceutical Bulletin  (Chemical & Pharmaceutical Bulletin)
Volume： 49  Issue： 9  Page： 1102-1109  Publication year： Sep. 01, 2001 
JST Material Number： G0504A  ISSN： 0009-2363  CODEN： CPBTAL  Document type： Article
Article type： 原著論文  Country of issue： Japan (JPN)  Language： ENGLISH (EN)

Thesaurus term： *nitrogen heterocyclic compound ,...

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JST classification (2)： Other 5-membered rings with two or more hetero atoms  (CF07085F) ,  Synthesis of drugs  (GV01030F)

Substance index (22)： TAK-456 ,  TAK-457 ,  1-[(2R,3R)-2-Hydroxy-2-(2,4-difluorophenyl)-3-[2-oxo-3-[4-(1H-tetrazole-1-yl)phenyl]-1-imidazolidinyl]butyl]-4-(isobutyryloxymethyl)-1H-1,2,4-triazole-4-ium ,  1-[(2R,3R)-2-Hydroxy-2-(2,4-difluorophenyl)-3-[2-oxo-3-[4-(1H-tetrazole-1-yl)phenyl]-1-imidazolidinyl]butyl]-4-(pivaloyloxymethyl)-1H-1,2,4-triazole-4-ium ,  1-[(2R,3R)-2-Hydroxy-2-(2,4-difluorophenyl)-3-[2-oxo-3-[4-(1H-tetrazole-1-yl)phenyl]-1-imidazolidinyl]butyl]-4-(ethoxycarbonyloxymethyl)-1H-1,2,4-triazole-4-ium ,  1-[(2R,3R)-2-Hydroxy-2-(2,4-difluorophenyl)-3-[2-oxo-3-[4-(1H-tetrazole-1-yl)phenyl]-1-imidazolidinyl]butyl]-4-(propoxycarbonyloxymethyl)-1H-1,2,4-triazole-4-ium ,  1-[(2R,3R)-2-Hydroxy-2-(2,4-difluorophenyl)-3-[2-oxo-3-[4-(1H-tetrazole-1-yl)phenyl]-1-imidazolidinyl]butyl]-4-(isopropoxycarbonyloxymethyl)-1H-1,2,4-triazole-4-ium ,  1-[(2R,3R)-2-Hydroxy-2-(2,4-difluorophenyl)-3-[2-oxo-3-[4-(1H-tetrazole-1-yl)phenyl]-1-imidazolidinyl]butyl]-4-(1,3-dioxane-5-yloxycarbonyloxymethyl)-1H-1,2,4-triazole-4-ium ,  1-[(2R,3R)-2-Hydroxy-2-(2,4-difluorophenyl)-3-[2-oxo-3-[4-(1H-tetrazole-1-yl)phenyl]-1-imidazolidinyl]butyl]-4-(3-hydroxypropoxycarbonyloxymethyl)-1H-1,2,4-triazole-4-ium ,  1-[(2R,3R)-2-Hydroxy-2-(2,4-difluorophenyl)-3-[2-oxo-3-[4-(1H-tetrazole-1-yl)phenyl]-1-imidazolidinyl]butyl]-4-(2-(acetylamino)ethoxycarbonyloxymethyl)-1H-1,2,4-triazole-4-ium ,  1-[(2R,3R)-2-Hydroxy-2-(2,4-difluorophenyl)-3-[2-oxo-3-[4-(1H-tetrazole-1-yl)phenyl]-1-imidazolidinyl]butyl]-4-methyl-1H-1,2,4-triazole-4-ium ,  Acetic acid chloromethyl ,  Acetic acid bromomethyl ,  Acetic acid iodomethyl ester ,  Isobutyric acid chloromethyl ester ,  Pivalic acid chloromethyl ,  Carbonic acid ethylchloromethyl ester ,  Carbonic acid propylchloromethyl ester ,  Carbonic acid isopropylchloromethyl ester ,  Carbonic acid 1,3-dioxane-5-ylchloromethyl ester ,  Carbonic acid 3-hydroxypropylchloromethyl ester ,  Carbonic acid 2-(acetylamino)ethylchloromethyl ester

Reference (31)：

• 1) Part XI: Ichikawa T., Kitazaki T., Matsushita Y., Hosono H., Yamada M., Mizuno M., Itoh K., Chem. Pharm. Bull., 48, 1947-1953 (2000).
• 2) Kitazaki T., Ichikawa T., Tasaka A., Hosono H., Matsushita Y., Hayashi R., Okonogi K., Itoh K., Chem. Pharm. Bull., 48, 1935-1946 (2000).
• 3) Tsuchimori N., Hayashi R., Kitamoto N., Asai K., Kitazaki T., Iizawa Y., Itoh K., Okonogi K., Antimicrob. Agents Chemother., submitted.
• 4) a) Graybill J.R., Eur. J. Clin. Infect. Dis., 8, 402-412 (1989)
•  b) Petit C., Cheron M., Joly V., Rodrigues J.M., Bolard J., Gaboriau F., J. Antimicrob. Chemother., 42, 779-785 (1998)

Terms in the title (10)： 光学活性 ,  抗真菌性 ,  アゾール類 ,  トリアゾール ,  ピル ,  フェニル ,  2-イミダゾリジノン ,  水溶性 ,  プロドラッグ ,  抗真菌活性