title: [Salicylic acid derivatives as simplified and novel GK small molecule activators].
abstract: Glucokinase (GK) is a new target for the treatment of type II diabetes mellitus (T2DM). In order to find a structure-simplified small molecule GK activator, 19 salicylic acid derivatives were designed and synthesized based on new lead compound (1). Experimental results showed that the potency of compound 8h is superior to control RO-28-0450 in GK activation.
authors.affiliation: Beijing Key Laboratory of Active Substance Discovery and Druggability Evaluation, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China.
authors.forename: Lian-Chao
authors.initials: LC
authors.lastname: Huo
authors.forename: Yu-Liang
authors.initials: YL
authors.lastname: Zhang
authors.forename: Lei
authors.initials: L
authors.lastname: Lei
authors.forename: Shuai-Nan
authors.initials: SN
authors.lastname: Liu
authors.forename: Zhu-Fang
authors.initials: ZF
authors.lastname: Shen
authors.forename: Yu-Ling
authors.initials: YL
authors.lastname: Wang
authors.forename: Hong-Rui
authors.initials: HR
authors.lastname: Song
authors.forename: Zhi-Qiang
authors.initials: ZQ
authors.lastname: Feng
mesh_terms: D015195:Drug Design; D004789:Enzyme Activation / Q000187:drug effects; D020536:Enzyme Activators / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D005941:Glucokinase / Q000378:metabolism*; D007004:Hypoglycemic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D015394:Molecular Structure; D012459:Salicylates / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013844:Thiazoles / Q000494:pharmacology
chemical_list: D020536:Enzyme Activators; D007004:Hypoglycemic Agents; C476008:RO-28-0450; D012459:Salicylates; D013844:Thiazoles; D005941:Glucokinase