FR131535, a novel water-soluble echinocandin-like lipopeptide: synthesis and biological properties.
The synthesis and biological properties of a novel water-soluble echinocandin-like lipopeptide, FR131535, are described. This compound displayed potent in vitro and in vivo antifungal activities. The hemolytic activity of FR901379 was reduced by replacing the acyl side chain. This compound showed good water-solubility, comparable to the natural product FR901379.
Fujie
A
A
Exploratory Research Laboratories, Fujisawa Pharmaceutical Co., Ltd., Ibaraki, Japan. akihiko_fujie@po.fujisawa.co.jp
Iwamoto
T
T
Sato
B
B
Muramatsu
H
H
Kasahara
C
C
Furuta
T
T
Hori
Y
Y
Hino
M
M
Hashimoto
S
S
D000818:Animals; D000900:Anti-Bacterial Agents / Q000737:chemistry / Q000494:pharmacology; D000935:Antifungal Agents / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D001994:Bronchogenic Cyst / Q000188:drug therapy; D002176:Candida albicans / Q000187:drug effects / Q000201:enzymology; D002177:Candidiasis / Q000188:drug therapy; D004195:Disease Models, Animal; D054714:Echinocandins; D005260:Female; D005656:Fungal Proteins; D005964:Glucosyltransferases / Q000037:antagonists & inhibitors*; D006461:Hemolysis / Q000187:drug effects; D008565:Membrane Proteins; D051379:Mice; D008819:Mice, Nude; D010455:Peptides; D010456:Peptides, Cyclic / Q000138:chemical synthesis / Q000494:pharmacology* / Q000633:toxicity; D011020:Pneumonia, Pneumocystis / Q000188:drug therapy; D029702:Schizosaccharomyces pombe Proteins; D012995:Solubility
D000900:Anti-Bacterial Agents; D000935:Antifungal Agents; D054714:Echinocandins; C110369:FR 131535; D005656:Fungal Proteins; D008565:Membrane Proteins; D010455:Peptides; D010456:Peptides, Cyclic; D029702:Schizosaccharomyces pombe Proteins; C007572:echinocandin B; D005964:Glucosyltransferases; C020570:1,3-beta-glucan synthase