title: Synthesis and structure-activity relationships of novel fungal chitin synthase inhibitors.
abstract: A novel Candida albicans chitin synthase 1 (CaChs1) inhibitor, RO-41-0986 (1) was discovered by random screening. Systematic modification led to the identification of a highly potent CaChs1 inhibitor, RO-09-3024 (2), having strong antifungal activity against Candida spp. in vitro.
authors.affiliation: Department of Chemistry, Nippon Roche Research Center, Kamakura, Kanagawa, Japan.
authors.forename: K
authors.initials: K
authors.lastname: Masubuchi
authors.forename: M
authors.initials: M
authors.lastname: Taniguchi
authors.forename: I
authors.initials: I
authors.lastname: Umeda
authors.forename: K
authors.initials: K
authors.lastname: Hattori
authors.forename: H
authors.initials: H
authors.lastname: Suda
authors.forename: Y
authors.initials: Y
authors.lastname: Kohchi
authors.forename: Y
authors.initials: Y
authors.lastname: Isshiki
authors.forename: T
authors.initials: T
authors.lastname: Sakai
authors.forename: M
authors.initials: M
authors.lastname: Kohchi
authors.forename: M
authors.initials: M
authors.lastname: Shirai
authors.forename: H
authors.initials: H
authors.lastname: Okabe
authors.forename: M
authors.initials: M
authors.lastname: Sudoh
authors.forename: T
authors.initials: T
authors.lastname: Yamazaki
authors.forename: N
authors.initials: N
authors.lastname: Shimma
mesh_terms: D000818:Animals; D000935:Antifungal Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D001232:Aspergillus fumigatus / Q000201:enzymology; D001577:Benzophenones / Q000138:chemical synthesis*; D002175:Candida / Q000201:enzymology*; D002687:Chitin Synthase / Q000037:antagonists & inhibitors*; D003454:Cryptococcus / Q000201:enzymology; D015195:Drug Design; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D051379:Mice; D015394:Molecular Structure; D013329:Structure-Activity Relationship
chemical_list: D000935:Antifungal Agents; D001577:Benzophenones; D004791:Enzyme Inhibitors; C415226:RO-09-3024; D002687:Chitin Synthase