Novel galbonolide derivatives as IPC synthase inhibitors: design, synthesis and in vitro antifungal activities.
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.
Sakoh
Hiroki
H
Banyu Tsukuba Research Institute, Okubo-3, Tsukuba 300-2611, Ibaraki, Japan.
Sugimoto
Yuichi
Y
Imamura
Hideaki
H
Sakuraba
Shunji
S
Jona
Hideki
H
Bamba-Nagano
Rie
R
Yamada
Koji
K
Hashizume
Terutaka
T
Morishima
Hajime
H
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*
D000935:Antifungal Agents; D007783:Lactones; C047784:rustmicin; D006602:Hexosyltransferases; C088714:phosphatidylinositol-ceramide phosphoinositol transferase