Glycogen phosphorylase a inhibitors with a phenethylphenylphthalimide skeleton derived from thalidomide-related alpha-glucosidase inhibitors and liver X receptor antagonists.
Novel glycogen phosphorylase a (GPa) inhibitors with a phenethylphenylphthalimide skeleton were prepared based on alpha-glucosidase inhibitors and liver X receptor (LXR) antagonists derived from thalidomide. Their structure-activity relationships were analyzed. Some of the compounds thus prepared showed potent inhibitory activity against rabbit muscle GPa with more than 10-fold greater efficacy than a typical GPa inhibitor, 1,4-dideoxy-1,4-imino-D-arabinitol.
Motoshima
Kazunori
K
Institute of Molecular & Cellular Biosciences, The University of Tokyo, Yayoi, Bunkyo-ku, Japan.
Ishikawa
Minoru
M
Sugita
Kazuyuki
K
Hashimoto
Yuichi
Y
D000818:Animals; D004791:Enzyme Inhibitors / Q000737:chemistry* / Q000494:pharmacology; D025001:Glycogen Phosphorylase, Liver Form / Q000037:antagonists & inhibitors* / Q000737:chemistry; D024982:Glycogen Phosphorylase, Muscle Form / Q000037:antagonists & inhibitors* / Q000737:chemistry; D065089:Glycoside Hydrolase Inhibitors; D000071518:Liver X Receptors; D057093:Orphan Nuclear Receptors / Q000037:antagonists & inhibitors* / Q000737:chemistry; D010797:Phthalimides / Q000138:chemical synthesis* / Q000494:pharmacology; D011817:Rabbits; D013792:Thalidomide / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology*
D004791:Enzyme Inhibitors; D065089:Glycoside Hydrolase Inhibitors; D000071518:Liver X Receptors; D057093:Orphan Nuclear Receptors; D010797:Phthalimides; D013792:Thalidomide; C037430:N-phenylphthalimide; D025001:Glycogen Phosphorylase, Liver Form; D024982:Glycogen Phosphorylase, Muscle Form