title: 2-O-carboxymethylpyrogallol derivatives as PTP1B inhibitors with antihyperglycemic activity.
abstract: 2-O-carboxymethylpyrogallol derivatives (4-17) were synthesized, with their in vitro inhibitory activities against PTP1B and in vivo antihyperglycemic effects examined. Compound 14, the most potent among the series, showed a K(i) value of 1.1 microM against PTP1B, 7-fold lower than that against TC-PTP. When compound 14 was fed to a high-fat diet-induced diabetic mouse model, significant improvements were observed in both the fasting glucose level and glucose tolerance.
authors.affiliation: Department of Chemistry and Institute of Molecular Cell Biology, Inha University, Incheon 402-751, Republic of Korea.
authors.forename: Bharat Raj
authors.initials: BR
authors.lastname: Bhattarai
authors.forename: Suja
authors.initials: S
authors.lastname: Shrestha
authors.forename: Seung Wook
authors.initials: SW
authors.lastname: Ham
authors.forename: Kwang Rok
authors.initials: KR
authors.lastname: Kim
authors.forename: Hyae Gyeong
authors.initials: HG
authors.lastname: Cheon
authors.forename: Keun-Hyeung
authors.initials: KH
authors.lastname: Lee
authors.forename: Hyeongjin
authors.initials: H
authors.lastname: Cho
mesh_terms: D000818:Animals; D001786:Blood Glucose / Q000378:metabolism; D002463:Cell Membrane Permeability / Q000187:drug effects; D003924:Diabetes Mellitus, Type 2 / Q000188:drug therapy; D004041:Dietary Fats; D005951:Glucose Tolerance Test; D006943:Hyperglycemia / Q000188:drug therapy*; D007004:Hypoglycemic Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D007333:Insulin Resistance; D007700:Kinetics; D008297:Male; D051379:Mice; D008810:Mice, Inbred C57BL; D017027:Protein Tyrosine Phosphatases / Q000037:antagonists & inhibitors; D013329:Structure-Activity Relationship
chemical_list: D001786:Blood Glucose; D004041:Dietary Fats; D007004:Hypoglycemic Agents; D017027:Protein Tyrosine Phosphatases