FK-463 Fujisawa Pharmaceutical Co Ltd

A. H. Groll, T. J. Walsh

Research output: Contribution to journalReview articlepeer-review


Novel cyclohexapeptides, pharmaceutically acceptable salts thereof, a process for preparing them and their use for the treatment of microbial infections, especially fungal infections including Pneumocystis carinii infection are claimed. The compounds are slated to be β-1,3-glucan synthase inhibitors and possess antimicrobial and antifungal activities. The in vitro antimicrobial activity was assessed against Candida albicans F6-633. The specified compound showed a MIC value of 0.1 μg/ml. Four schemes and 32 examples detail the syntheses of the compounds. Characterization is by 1H-NMR, MS and elemental analysis data. 119 Intermediates are also exemplified and characterized by 1-NMR and MS data. No compounds are specifically claimed. The specified compound is, des(N-10,12-dimethyltetradecanoyl)-N-(4-[2-(4-butoxyphenyl)-1,3,4-thiadiazol-5-y l]benzoyl)-4-[6-(3-hy droxy-4-methylproline)-4-(3-sulfooxy-4-hydroxyphenyl)-4-hydroxythreonine]pneumoc andin BO with unspecified stereochemistry.

Original languageEnglish (US)
Pages (from-to)405-412
Number of pages8
JournalCurrent Opinion in Anti-infective Investigational Drugs
Issue number4
StatePublished - 2000

ASJC Scopus subject areas

  • Pharmacology
  • Microbiology (medical)


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