FK-463 Fujisawa Pharmaceutical Co Ltd

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.