title: Non-competitive and selective dipeptidyl peptidase IV inhibitors with phenethylphenylphthalimide skeleton derived from thalidomide-related α-glucosidase inhibitors and liver X receptor antagonists.
abstract: Novel dipeptidyl peptidase IV (DPP-IV) inhibitors with a phenethylphenylphthalimide skeleton were prepared based on α-glucosidase inhibitors and liver X receptor (LXR) antagonists derived from thalidomide. Representative compounds showed non-competitive inhibition of DPP-IV and 28a exhibited 10-fold selectivity for DPP-IV over DPP-8. Compound 28a is the first non-competitive, selective DPP-IV inhibitor.
authors.affiliation: Institute of Molecular and Cellular Biosciences, The University of Tokyo, 1-1-1 Yayoi, Tokyo 113-0032, Japan.
authors.forename: Kazunori
authors.initials: K
authors.lastname: Motoshima
authors.forename: Kazuyuki
authors.initials: K
authors.lastname: Sugita
authors.forename: Yuichi
authors.initials: Y
authors.lastname: Hashimoto
authors.forename: Minoru
authors.initials: M
authors.lastname: Ishikawa
mesh_terms: D001667:Binding, Competitive; D054873:Dipeptidyl-Peptidase IV Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D004789:Enzyme Activation / Q000187:drug effects*; D065089:Glycoside Hydrolase Inhibitors; D020128:Inhibitory Concentration 50; D007700:Kinetics; D000071518:Liver X Receptors; D015394:Molecular Structure; D057093:Orphan Nuclear Receptors / Q000037:antagonists & inhibitors*; D010797:Phthalimides / Q000737:chemistry*; D013792:Thalidomide / Q000737:chemistry*; D000520:alpha-Glucosidases
chemical_list: D054873:Dipeptidyl-Peptidase IV Inhibitors; D065089:Glycoside Hydrolase Inhibitors; D000071518:Liver X Receptors; D057093:Orphan Nuclear Receptors; D010797:Phthalimides; D013792:Thalidomide; D000520:alpha-Glucosidases