Structure-activity relationships of phomactin derivatives as platelet activating factor antagonists.
Phomactins, natural products isolated from the culture broth of marine fungus Phoma sp., were found to be active as PAF antagonists. This unique carbon skeleton led us to investigate the structure-activity relationship demonstrating that the lipophilicity at C-(7-8), acetoxy, (methoxycarbonyl)oxy, and 3-isoxazolyloxy substitution at C-20, and 2-beta-OH configuration at C-2 are all required for the enhancement of inhibitor activity.
Sugano
M
M
Biomedical Research Laboratories, Sankyo Co. Ltd, Tokyo, Japan.
Sato
A
A
Saito
K
K
Takaishi
S
S
Matsushita
Y
Y
Iijima
Y
Y
D004852:Epoxy Compounds / Q000737:chemistry* / Q000494:pharmacology*; D009682:Magnetic Resonance Spectroscopy; D010972:Platelet Activating Factor / Q000037:antagonists & inhibitors*; D011869:Radioligand Assay; D013329:Structure-Activity Relationship
D004852:Epoxy Compounds; D010972:Platelet Activating Factor; C103093:phomactin D