Art

J-GLOBAL ID：200902299057273108   Reference number：03A0132546

Design, Synthesis and Antifungal Activity of a Novel Water Soluble Prodrug of Antifungal Triazole.

抗真菌性トリアゾールの新規水溶性プロドラッグの設計,合成及び抗真菌作用

Author (9)： OHWADA J (Nippon Roche Res. Center, Kanagawa, JPN) ,  TSUKAZAKI M (Nippon Roche Res. Center, Kanagawa, JPN) ,  HAYASE T (Nippon Roche Res. Center, Kanagawa, JPN) ,  OIKAWA N (Nippon Roche Res. Center, Kanagawa, JPN) ,  ISSHIKI Y (Nippon Roche Res. Center, Kanagawa, JPN) ,  FUKUDA H (Nippon Roche Res. Center, Kanagawa, JPN) ,  MIZUGUCHI E (Nippon Roche Res. Center, Kanagawa, JPN) ,  SAKAITANI M (Nippon Roche Res. Center, Kanagawa, JPN) ,  SHIMMA N (Nippon Roche Res. Center, Kanagawa, JPN)
Material： Bioorganic & Medicinal Chemistry Letters  (Bioorg Med Chem Lett)
Volume： 13  Issue： 2  Page： 191-196  Publication year： Jan. 20, 2003 
JST Material Number： W0248A  ISSN： 0960-894X  Document type： Article
Article type： 短報  Country of issue： Netherlands (NLD)  Language： ENGLISH (EN)

Thesaurus term： *nitrogen heterocyclic compound ,...

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JST classification (2)： Triazoles  (CF07084O) ,  Synthesis of drugs  (GV01030F)

Substance index (32)： 1-[(2R,3R)-2-(2,5-Difluorophenyl)-2-hydroxy-3-[4-(4-cyanophenyl)thiazole-2-yl]butyl]-4-[1-[methyl[3-[[(methylamino)acetoxy]methyl]-2-pyridyl]carbamoyloxy]ethyl]-1H-1,2,4-triazole-4-ium ,  RO-0098557 ,  RO-0094815 ,  1-[(2R,3R)-2-Hydroxy-2-(2,5-difluorophenyl)-3-[4-(4-cyanophenyl)-2-thiazolyl]butyl]-4-[N-methyl-N-(3-acetoxypropyl)carbamoyloxymethyl]-1H-1,2,4-triazole-4-ium ,  1-[(2R,3R)-2-Hydroxy-2-(2,5-difluorophenyl)-3-[4-(4-cyanophenyl)-2-thiazolyl]butyl]-4-[N-methyl-N-(3-hydroxypropyl)carbamoyloxymethyl]-1H-1,2,4-triazole-4-ium ,  3-Methyltetrahydro-2H-1,3-oxazin-2-one ,  Formaldehyde ,  N-Methylaniline ,  N-Methyl-N-phenylcarbamic acid chloromethyl ester ,  1-[(2R,3R)-2-Hydroxy-2-(2,5-difluorophenyl)-3-[4-(4-cyanophenyl)-2-thiazolyl]butyl]-4-(N-methyl-N-phenylcarbamoyloxymethyl)-1H-1,2,4-triazole-4-ium ,  2-(Methylamino)ethanol ,  N-Methyl-N-(2-acetoxyethyl)carbamic acid chloromethyl ester ,  1-[(2R,3R)-2-Hydroxy-2-(2,5-difluorophenyl)-3-[4-(4-cyanophenyl)-2-thiazolyl]butyl]-4-[N-methyl-N-(2-acetoxyethyl)carbamoyloxymethyl]-1H-1,2,4-triazole-4-ium ,  1-[(2R,3R)-2-Hydroxy-2-(2,5-difluorophenyl)-3-[4-(4-cyanophenyl)-2-thiazolyl]butyl]-4-[N-methyl-N-(3-acetoxypropyl)carbamoyloxymethyl]-1H-1,2,4-triazole-4-ium・iodide ,  1-[(2R,3R)-2-Hydroxy-2-(2,5-difluorophenyl)-3-[4-(4-cyanophenyl)-2-thiazolyl]butyl]-4-[[(2S)-2α-(acetoxymethyl)pyrrolizino]carbonyloxymethyl]-1H-1,2,4-triazole-4-ium ,  1-[(2R,3R)-2-Hydroxy-2-(2,5-difluorophenyl)-3-[4-(4-cyanophenyl)-2-thiazolyl]butyl]-4-[[(2S)-2α-(acetoxymethyl)pyrrolizino]carbonyloxymethyl]-1H-1,2,4-triazole-4-ium・iodide ,  1-[(2R,3R)-2-Hydroxy-2-(2,5-difluorophenyl)-3-[4-(4-cyanophenyl)-2-thiazolyl]butyl]-4-[N-methyl-N-[2-(acetoxymethyl)phenyl]carbamoyloxymethyl]-1H-1,2,4-triazole-4-ium ,  1-[(2R,3R)-2-Hydroxy-2-(2,5-difluorophenyl)-3-[4-(4-cyanophenyl)-2-thiazolyl]butyl]-4-[N-methyl-N-[2-(acetoxymethyl)phenyl]carbamoyloxymethyl]-1H-1,2,4-triazole-4-ium・chloride ,  2-Chloronicotinic acid ,  2-Chloro-3-pyridinecarboxylic acid tert-butyl ester ,  2-(Methylamino)-3-pyridinecarboxylic acid tert-butyl ester ,  2-(Methylamino)-3-pyridinemethanol ,  N-Methyl-N-[3-[[[methyl(tert-butoxycarbonyl)amino]acetoxy]methyl]-2-pyridyl]carbamic acid 1-chloroethyl ester ,  1-[(2R,3R)-2-Hydroxy-2-(2,5-difluorophenyl)-3-[4-(4-cyanophenyl)-2-thiazolyl]butyl]-4-[1-[N-methyl-N-[3-[[[methyl(tert-butoxycarbonyl)amino]acetoxy]methyl]-2-pyridyl]carbamoyloxy]ethyl]-1H-1,2,4-triazole-4-ium ,  1-[(2R,3R)-2-Hydroxy-2-(2,5-difluorophenyl)-3-[4-(4-cyanophenyl)-2-thiazolyl]butyl]-4-[1-[N-methyl-N-[2-[[(methylamino)acetoxy]methyl]-4,5-difluorophenyl]carbamoyloxy]ethyl]-1H-1,2,4-triazole-4-ium ,  1-[(2R,3R)-2-Hydroxy-2-(2,5-difluorophenyl)-3-[4-(4-cyanophenyl)-2-thiazolyl]butyl]-4-[1-[N-methyl-N-[2-[[(methylamino)acetoxy]methyl]-4,5-difluorophenyl]carbamoyloxy]ethyl]-1H-1,2,4-triazole-4-ium・chloride・hydrochloride ,  1-[(2R,3R)-2-Hydroxy-2-(2,5-difluorophenyl)-3-[4-(4-cyanophenyl)-2-thiazolyl]butyl]-4-[1-[N-methyl-N-[2-[[(methylamino)acetoxy]methyl]-3-fluorophenyl]carbamoyloxy]ethyl]-1H-1,2,4-triazole-4-ium ,  1-[(2R,3R)-2-Hydroxy-2-(2,5-difluorophenyl)-3-[4-(4-cyanophenyl)-2-thiazolyl]butyl]-4-[1-[N-methyl-N-[2-[[(methylamino)acetoxy]methyl]-3-fluorophenyl]carbamoyloxy]ethyl]-1H-1,2,4-triazole-4-ium・chloride・hydrochloride ,  1-[(2R,3R)-2-Hydroxy-2-(2,5-difluorophenyl)-3-[4-(4-cyanophenyl)-2-thiazolyl]butyl]-4-[1-[N-methyl-N-[2-[[(methylamino)acetoxy]methyl]-4-fluorophenyl]carbamoyloxy]ethyl]-1H-1,2,4-triazole-4-ium ,  1-[(2R,3R)-2-Hydroxy-2-(2,5-difluorophenyl)-3-[4-(4-cyanophenyl)-2-thiazolyl]butyl]-4-[1-[N-methyl-N-[2-[[(methylamino)acetoxy]methyl]-4-fluorophenyl]carbamoyloxy]ethyl]-1H-1,2,4-triazole-4-ium・chloride・hydrochloride ,  1-[(2R,3R)-2-Hydroxy-2-(2,5-difluorophenyl)-3-[4-(4-cyanophenyl)-2-thiazolyl]butyl]-4-[1-[N-methyl-N-[2-[[(methylamino)acetoxy]methyl]-5-chlorophenyl]carbamoyloxy]ethyl]-1H-1,2,4-triazole-4-ium ,  1-[(2R,3R)-2-Hydroxy-2-(2,5-difluorophenyl)-3-[4-(4-cyanophenyl)-2-thiazolyl]butyl]-4-[1-[N-methyl-N-[2-[[(methylamino)acetoxy]methyl]-5-chlorophenyl]carbamoyloxy]ethyl]-1H-1,2,4-triazole-4-ium・chloride・hydrochloride

Terms in the title (6)： 抗真菌性 ,  トリアゾール ,  水溶性 ,  プロドラッグ ,  設計 ,  抗真菌作用