fr-901469 has been researched along with Candidiasis* in 4 studies
4 other study(ies) available for fr-901469 and Candidiasis
| Article | Year |
|---|---|
Synthesis and biological activity of novel macrocyclic antifungals: acylated conjugates of the ornithine moiety of the lipopeptidolactone FR901469.
A series of acylated analogues of the novel macrocyclic lipopeptidolactone FR901469 has been prepared and evaluated for antifungal and hemolytic activity. Several analogues displayed markedly reduced hemolytic potential and comparable protective effects to the natural product in a mouse model of candidiasis. Topics: Animals; Antifungal Agents; Candidiasis; Depsipeptides; Hemolysis; Mice; Mice, Inbred ICR; Peptides, Cyclic; Structure-Activity Relationship | 2001 |
Synthesis and biological activity of novel macrocyclic antifungals. modification of the tyrosine moiety of the lipopeptidolactone FR901469.
A series of tyrosine-modified derivatives of the macrocyclic lipopeptidolactone FR901469 have been prepared and evaluated for in vitro and in vivo antifungal activity and for hemolytic activity towards red blood cells. Compound 14 displayed significantly reduced hemolytic potential at 1mg/mL and a comparable protective effect to FR901469 in a mouse candidiasis model. Topics: Animals; Antifungal Agents; Candida albicans; Candidiasis; Depsipeptides; Erythrocytes; Hemolysis; Lactones; Mice; Microbial Sensitivity Tests; Peptides, Cyclic; Tyrosine | 2001 |
Novel amidine conjugates of the ornithine moiety of the macrocyclic antifungal lipopeptidolactone FR901469.
Topics: Amidines; Animals; Antifungal Agents; Aspergillus fumigatus; Candida; Candidiasis; Chromatography, High Pressure Liquid; Depsipeptides; Hemolysis; Magnetic Resonance Spectroscopy; Mice; Microbial Sensitivity Tests; Ornithine; Peptides, Cyclic; Spectrometry, Mass, Fast Atom Bombardment; Spectrophotometry, Infrared | 2001 |
FR901469, a novel antifungal antibiotic from an unidentified fungus No.11243. II. In vitro and in vivo activities.
FR901469 is a water-soluble macrocyclic lipopeptidolactone (C71H116N14O23) that has inhibitory activity against 1,3-beta-glucan synthase and exhibits in vitro and in vivo antifungal activity against both Candida albicans and Aspergillus fumigatus. The MICs of FR901469 against Candida albicans FP633 and Aspergillus fumigatus FP1305 in a micro-broth dilution test were 0.63 and 0.16 microg/ml, respectively. FR901469 showed excellent efficacy by subcutaneous injection against both Candida albicans and Aspergillus fumigatus in a murine systemic infection mode, with ED50s of 0.32 and 0.2 mg/kg, respectively. This compound also showed potent anti-Pneumocystis activity in the nude mice model with experimental Pneumocystis pneumonia. The hemolytic activity of FR901469 towards mouse red blood cells, is about 30-fold weaker than that of amphotericin B. Topics: Animals; Antifungal Agents; Aspergillosis; Aspergillus fumigatus; Candida albicans; Candidiasis; Depsipeptides; Disease Models, Animal; Female; Hemolysis; Mice; Mice, Inbred ICR; Mice, Nude; Microbial Sensitivity Tests; Peptides, Cyclic; Pneumocystis; Pneumonia, Pneumocystis; Treatment Outcome | 2000 |