Synthesis and antifungal activities of novel 1,3-β- d -glucan synthase inhibitors. Part 1

Autor: Takahide Watanabe, Toshikazu Yamazaki, Tomoaki Inoue, Yasuko Satoh, Kazuko Kobayashi, Kazunao Masubuchi, Takehiro Okada, Ikuo Horii, Eisaku Mizuguchi, Masahiro Aoki, Masahiro Sakaitani, Haruyoshi Shirai, Nobuo Shimma, Masami Kohchi, Osamu Kondoh
Rok vydání: 2001
Předmět:
Antifungal Agents
Clinical Biochemistry
Pharmaceutical Science
Microbial Sensitivity Tests
Biochemistry
Chemical synthesis
Microbiology
Aspergillus fumigatus
Inhibitory Concentration 50
Lactones
Mice
Structure-Activity Relationship
chemistry.chemical_compound
Candida albicans
Drug Discovery
medicine
Animals
Combinatorial Chemistry Techniques
Enzyme Inhibitors
Molecular Biology
Inclusion Bodies
Depsipeptide
chemistry.chemical_classification
biology
Chemistry
Organic Chemistry
Candidiasis
Membrane Proteins
Ornithine
medicine.disease
biology.organism_classification
Anti-Bacterial Agents
Survival Rate
Disease Models
Animal

Enzyme
Liver
Therapeutic Equivalency
Glucosyltransferases
Enzyme inhibitor
biology.protein
Molecular Medicine
Schizosaccharomyces pombe Proteins
Systemic candidiasis
Peptides
Zdroj: Bioorganic & Medicinal Chemistry Letters. 11:395-398
ISSN: 0960-894X
DOI: 10.1016/s0960-894x(00)00678-8
Popis: Highly potent 1,3-β- d -glucan synthase inhibitors, 7b , 10a , 10b and 12 , have been identified by the chemical modification of the ornithine residue of a fungicidal macrocyclic lipopeptidolactone, RO-09-3655 ( 1 ), isolated from the cultured broth of Deuteromycotinia spp. These compounds showed stronger antifungal activity against systemic candidiasis as well as pulmonary aspergillosis in mice, and less hepatotoxicity as compared with 1 .
Databáze: OpenAIRE