Synthesis and antifungal activities of novel 1,3-beta-D-glucan synthase inhibitors. Part 1.

Authors :: Masubuchi K
Okada T
Kohchi M
Sakaitani M
Mizuguchi E
Shirai H
Aoki M
Watanabe T
Kondoh O
Yamazaki T
Satoh Y
Kobayashi K
Inoue T
Horii I
Shimma N
Source :: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2001 Feb 12; Vol. 11 (3), pp. 395-8.
Publication Year :: 2001
Abstract: Highly potent 1,3-beta-D-glucan synthase inhibitors 10, 11 and 13 have been identified by the chemical modification of the fungicidal macrocyclic lipopeptidolactone, RO-09-3655 (1), isolated from the cultured broth of Deuteromycotinia spp. D-Ornithine derivative (10) showed improved antifungal activity in the systemic candidiasis model in mice and reduced hepatotoxicity in vitro, as compared with 1.

Subjects :: Animals
Anti-Bacterial Agents chemical synthesis
Anti-Bacterial Agents chemistry
Anti-Bacterial Agents pharmacology
Antifungal Agents chemistry
Candida albicans drug effects
Candidiasis complications
Candidiasis drug therapy
Combinatorial Chemistry Techniques
Disease Models, Animal
Enzyme Inhibitors chemical synthesis
Enzyme Inhibitors chemistry
Enzyme Inhibitors pharmacology
Inclusion Bodies drug effects
Inclusion Bodies microbiology
Inhibitory Concentration 50
Lactones chemical synthesis
Lactones chemistry
Lactones pharmacology
Liver drug effects
Liver microbiology
Liver pathology
Mice
Microbial Sensitivity Tests
Peptides
Structure-Activity Relationship
Survival Rate
Therapeutic Equivalency
Antifungal Agents chemical synthesis
Antifungal Agents pharmacology
Glucosyltransferases antagonists & inhibitors
Membrane Proteins
Schizosaccharomyces pombe Proteins

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