title: Discovery of Imigliptin, a Novel Selective DPP-4 Inhibitor for the Treatment of Type 2 Diabetes.
abstract: We report our discovery of a novel series of potent and selective dipeptidyl peptidase IV (DPP-4) inhibitors. Starting from a lead identified by scaffold-hopping approach, our discovery and development efforts were focused on exploring structure-activity relationships, optimizing pharmacokinetic profile, improving in vitro and in vivo efficacy, and evaluating safety profile. The selected candidate, Imigliptin, is now undergoing clinical trial.
authors.affiliation: Department of Project Management, Medicinal Chemistry, Process, Pharmacology, Drug Metabolism and Pharmacokenetics, Toxicology, XuanZhu Pharma , 2518 Tianchen Street, Jinan, Shandong, The People's Republic of China.
authors.forename: Chutian
authors.initials: C
authors.lastname: Shu
authors.affiliation: School of Pharmaceutical Sciences & Institute of Human Virology, Sun Yat-Sen University , 132 East Circle Road at University City, Guangzhou, The People's Republic of China.
authors.forename: Hu
authors.initials: H
authors.lastname: Ge
authors.affiliation: Department of Project Management, Medicinal Chemistry, Process, Pharmacology, Drug Metabolism and Pharmacokenetics, Toxicology, XuanZhu Pharma , 2518 Tianchen Street, Jinan, Shandong, The People's Republic of China.
authors.forename: Michael
authors.initials: M
authors.lastname: Song
authors.affiliation: Department of Project Management, Medicinal Chemistry, Process, Pharmacology, Drug Metabolism and Pharmacokenetics, Toxicology, XuanZhu Pharma , 2518 Tianchen Street, Jinan, Shandong, The People's Republic of China.
authors.forename: Jyun-Hong
authors.initials: JH
authors.lastname: Chen
authors.affiliation: Department of Project Management, Medicinal Chemistry, Process, Pharmacology, Drug Metabolism and Pharmacokenetics, Toxicology, XuanZhu Pharma , 2518 Tianchen Street, Jinan, Shandong, The People's Republic of China.
authors.forename: Huimin
authors.initials: H
authors.lastname: Zhou
authors.affiliation: Department of Project Management, Medicinal Chemistry, Process, Pharmacology, Drug Metabolism and Pharmacokenetics, Toxicology, XuanZhu Pharma , 2518 Tianchen Street, Jinan, Shandong, The People's Republic of China.
authors.forename: Qu
authors.initials: Q
authors.lastname: Qi
authors.affiliation: Department of Project Management, Medicinal Chemistry, Process, Pharmacology, Drug Metabolism and Pharmacokenetics, Toxicology, XuanZhu Pharma , 2518 Tianchen Street, Jinan, Shandong, The People's Republic of China.
authors.forename: Feng
authors.initials: F
authors.lastname: Wang
authors.affiliation: Department of Project Management, Medicinal Chemistry, Process, Pharmacology, Drug Metabolism and Pharmacokenetics, Toxicology, XuanZhu Pharma , 2518 Tianchen Street, Jinan, Shandong, The People's Republic of China.
authors.forename: Xifeng
authors.initials: X
authors.lastname: Ma
authors.affiliation: Department of Project Management, Medicinal Chemistry, Process, Pharmacology, Drug Metabolism and Pharmacokenetics, Toxicology, XuanZhu Pharma , 2518 Tianchen Street, Jinan, Shandong, The People's Republic of China.
authors.forename: Xiaolei
authors.initials: X
authors.lastname: Yang
authors.affiliation: Department of Project Management, Medicinal Chemistry, Process, Pharmacology, Drug Metabolism and Pharmacokenetics, Toxicology, XuanZhu Pharma , 2518 Tianchen Street, Jinan, Shandong, The People's Republic of China.
authors.forename: Genyan
authors.initials: G
authors.lastname: Zhang
authors.affiliation: Department of Project Management, Medicinal Chemistry, Process, Pharmacology, Drug Metabolism and Pharmacokenetics, Toxicology, XuanZhu Pharma , 2518 Tianchen Street, Jinan, Shandong, The People's Republic of China.
authors.forename: Yanwei
authors.initials: Y
authors.lastname: Ding
authors.affiliation: Department of Project Management, Medicinal Chemistry, Process, Pharmacology, Drug Metabolism and Pharmacokenetics, Toxicology, XuanZhu Pharma , 2518 Tianchen Street, Jinan, Shandong, The People's Republic of China.
authors.forename: Dapeng
authors.initials: D
authors.lastname: Zhou
authors.affiliation: Department of Project Management, Medicinal Chemistry, Process, Pharmacology, Drug Metabolism and Pharmacokenetics, Toxicology, XuanZhu Pharma , 2518 Tianchen Street, Jinan, Shandong, The People's Republic of China.
authors.forename: Peng
authors.initials: P
authors.lastname: Peng
authors.affiliation: Department of Project Management, Medicinal Chemistry, Process, Pharmacology, Drug Metabolism and Pharmacokenetics, Toxicology, XuanZhu Pharma , 2518 Tianchen Street, Jinan, Shandong, The People's Republic of China ; School of Pharmaceutical Sciences & Institute of Human Virology, Sun Yat-Sen University , 132 East Circle Road at University City, Guangzhou, The People's Republic of China.
authors.forename: Cheng-Kon
authors.initials: CK
authors.lastname: Shih
authors.affiliation: School of Pharmaceutical Sciences & Institute of Human Virology, Sun Yat-Sen University , 132 East Circle Road at University City, Guangzhou, The People's Republic of China.
authors.forename: Jun
authors.initials: J
authors.lastname: Xu
authors.affiliation: Department of Project Management, Medicinal Chemistry, Process, Pharmacology, Drug Metabolism and Pharmacokenetics, Toxicology, XuanZhu Pharma , 2518 Tianchen Street, Jinan, Shandong, The People's Republic of China ; School of Pharmaceutical Sciences & Institute of Human Virology, Sun Yat-Sen University , 132 East Circle Road at University City, Guangzhou, The People's Republic of China.
authors.forename: Frank
authors.initials: F
authors.lastname: Wu
keywords: Diabetes; OGTT; dipeptidyl peptidase IV (DPP-4); imigliptin; inhibitor; pyridinylimidazolone; scaffold-hopping