title: Synthesis and antifungal activities of novel 1,3-beta-D-glucan synthase inhibitors. Part 1.
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.
authors.affiliation: Department of Chemistry, Nippon Roche Research Center, Kanagawa, Japan.
authors.forename: K
authors.initials: K
authors.lastname: Masubuchi
authors.forename: T
authors.initials: T
authors.lastname: Okada
authors.forename: M
authors.initials: M
authors.lastname: Kohchi
authors.forename: M
authors.initials: M
authors.lastname: Sakaitani
authors.forename: E
authors.initials: E
authors.lastname: Mizuguchi
authors.forename: H
authors.initials: H
authors.lastname: Shirai
authors.forename: M
authors.initials: M
authors.lastname: Aoki
authors.forename: T
authors.initials: T
authors.lastname: Watanabe
authors.forename: O
authors.initials: O
authors.lastname: Kondoh
authors.forename: T
authors.initials: T
authors.lastname: Yamazaki
authors.forename: Y
authors.initials: Y
authors.lastname: Satoh
authors.forename: K
authors.initials: K
authors.lastname: Kobayashi
authors.forename: T
authors.initials: T
authors.lastname: Inoue
authors.forename: I
authors.initials: I
authors.lastname: Horii
authors.forename: N
authors.initials: N
authors.lastname: Shimma
mesh_terms: D000818:Animals; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D000935:Antifungal Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D002176:Candida albicans / Q000187:drug effects; D002177:Candidiasis / Q000150:complications / Q000188:drug therapy; D020650:Combinatorial Chemistry Techniques; D004195:Disease Models, Animal; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D005964:Glucosyltransferases / Q000037:antagonists & inhibitors*; D002479:Inclusion Bodies / Q000187:drug effects / Q000382:microbiology; D020128:Inhibitory Concentration 50; D007783:Lactones / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D008099:Liver / Q000187:drug effects / Q000382:microbiology / Q000473:pathology; D008565:Membrane Proteins; D051379:Mice; D008826:Microbial Sensitivity Tests; D010455:Peptides; D029702:Schizosaccharomyces pombe Proteins; D013329:Structure-Activity Relationship; D015996:Survival Rate; D013810:Therapeutic Equivalency
chemical_list: D000900:Anti-Bacterial Agents; D000935:Antifungal Agents; D004791:Enzyme Inhibitors; D007783:Lactones; D008565:Membrane Proteins; D010455:Peptides; D029702:Schizosaccharomyces pombe Proteins; D005964:Glucosyltransferases; C020570:1,3-beta-glucan synthase