title: Novel galbonolide derivatives as IPC synthase inhibitors: design, synthesis and in vitro antifungal activities.
abstract: A series of novel galbonolide derivatives having a modified methyl enol ether moiety were prepared in total synthetic procedures and evaluated for their in vitro antifungal activities. The antifungal activity was labile to modification of the enol ether functionality and almost all of the modified compounds lacked the activity except for the analogue with an introduction of a methylthio group at the C-6 position, which retained a modest antifungal potency against Cryptococcus neoformans.
authors.affiliation: Banyu Tsukuba Research Institute, Okubo-3, Tsukuba 300-2611, Ibaraki, Japan.
authors.forename: Hiroki
authors.initials: H
authors.lastname: Sakoh
authors.forename: Yuichi
authors.initials: Y
authors.lastname: Sugimoto
authors.forename: Hideaki
authors.initials: H
authors.lastname: Imamura
authors.forename: Shunji
authors.initials: S
authors.lastname: Sakuraba
authors.forename: Hideki
authors.initials: H
authors.lastname: Jona
authors.forename: Rie
authors.initials: R
authors.lastname: Bamba-Nagano
authors.forename: Koji
authors.initials: K
authors.lastname: Yamada
authors.forename: Terutaka
authors.initials: T
authors.lastname: Hashizume
authors.forename: Hajime
authors.initials: H
authors.lastname: Morishima
mesh_terms: D000935:Antifungal Agents / Q000737:chemistry* / Q000494:pharmacology*; D003455:Cryptococcus neoformans / Q000187:drug effects; D015195:Drug Design; D006602:Hexosyltransferases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D007783:Lactones / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: D000935:Antifungal Agents; D007783:Lactones; C047784:rustmicin; D006602:Hexosyltransferases; C088714:phosphatidylinositol-ceramide phosphoinositol transferase