In vitro antifungal activity of novel azole derivatives with a morpholine ring, UR-9746 and UR-9751, and comparison with fluconazole.
Thirty-three patient fungal isolates were studied by broth macrodilution methods for susceptibility to novel azole derivatives with a morpholine ring, UR-9746 and UR-9751, and fluconazole. MICs (micrograms/ml) ranged widely, but none had lower MICs for Candida albicans or Cryptococcus neoformans than UR-9751. Fluconazole and UR-9751 had the most activity versus other Candida species. Activity was demonstrated versus endemic fungal pathogens. Aspergillus species were generally resistant, although modest activity was seen. UR-9746 and UR-9751 are active in vitro, with a potency comparable to that of fluconazole.
Stevens
D A
DA
Department of Medicine, Santa Clara Valley Medical Center, San Jose, CA 95128-2699, USA.
Aristizabal
B H
BH
D000935:Antifungal Agents / Q000494:pharmacology* / Q000627:therapeutic use; D003470:Culture Media; D015725:Fluconazole / Q000494:pharmacology* / Q000627:therapeutic use; D005658:Fungi / Q000187:drug effects* / Q000302:isolation & purification; D006801:Humans; D008826:Microbial Sensitivity Tests; D009025:Morpholines / Q000494:pharmacology* / Q000627:therapeutic use; D009181:Mycoses / Q000188:drug therapy; D014230:Triazoles / Q000494:pharmacology* / Q000627:therapeutic use
D000935:Antifungal Agents; D003470:Culture Media; D009025:Morpholines; D014230:Triazoles; C104730:UR 9746; C104729:UR 9751; D015725:Fluconazole