Synthesis of 1233A analogs and their inhibitory activity against hydroxymethylglutaryl coenzyme A synthase.
Simple and efficient syntheses of 1233A analogs were developed and the inhibitory activity of the analogs against hydroxymethylglutaryl coenzyme A (HMG-CoA) synthase was determined. Study of the structure-activity relationships revealed that not only the geometry in beta-lactone moiety but also the length of the carbon side chain is important for inhibitory activity against HMG-CoA synthase.
Research Center for Biological Function, Kitasato Institute, Tokyo, Japan.
T
T
Sunazuka
K
K
Tsuzuki
H
H
Kumagai
H
H
Tomoda
H
H
Tanaka
H
H
Nagashima
H
H
Hashizume
S
S
Omura
D000818:Animals; D005231:Fatty Acids, Unsaturated / Q000138:chemical synthesis* / Q000494:pharmacology; D006904:Hydroxymethylglutaryl-CoA Synthase / Q000037:antagonists & inhibitors*; D007783:Lactones / Q000138:chemical synthesis* / Q000494:pharmacology; D008798:Mevalonic Acid / Q000031:analogs & derivatives / Q000494:pharmacology; D008826:Microbial Sensitivity Tests; D014709:Vero Cells / Q000187:drug effects
D005231:Fatty Acids, Unsaturated; D007783:Lactones; C054282:antibiotic 1233A; C015367:mevalonolactone; D006904:Hydroxymethylglutaryl-CoA Synthase; D008798:Mevalonic Acid