Design, Synthesis and SAR Studies of Novel and Potent Dipeptidyl Peptidase 4 Inhibitors

作     者：Na Luo Xiaoyu Fang Mingbo Su Xinwen Zhang Dan Li Honglin Li Shiliang Li Zhenjiang Zhao Na Luo;Xiaoyu Fang;Mingbo Su;Xinwen Zhang;Dan Li;Honglin Li;Shiliang Li;Zhenjiang Zhao

作者机构：Shanghai Key Laboratory of New Drug DesignSchool of PharmacyEast China University of Science and Technology130 Meilong RoadShanghai 200237China State Key Laboratory of Drug ResearchShanghai Institute of Materia MedicaChinese Academy of Sciences555 Zhuchongzhi RoadShanghai 201203China Shandong Biopolar Dichang Pharmaceutical Co.LtdRM2306No.786 Linzi AvenueZiboShandong 255400China 

基　　金：This work was supported by the National Key Research and Development Program(No.2016YFA0502304 to H.L.) the National Natural Science Foundation of China(No.81825020 to H.L,No.81803437 to SL.) the National Science&Technology Major Project"Key New Drug Creation and Manufacturing Program",China(No.2018ZX09711002) the Fundamental Research Funds for the Central Universities,Special Program for Applied Research on Super Computation of the NSFC-Guangdong Joint Fund(the second phase)under Grant No.U1501501 Shiliang Li is sponsored by Shanghai Sailing Program(No.18YF1405100) Honglin Li is also sponsored by the National Program for Special Supports of Emi nent Professionals and the National Program for Support of Top-notch Young Professionals 

出 版 物：《Chinese Journal of Chemistry》 (中国化学（英文版）)

年 卷 期：2021年第39卷第1期

页      码：115-120页

摘      要：Dipeptidyl peptidase 4(DPP-4)is a clinically validated target for the treatment of type 2 diabetes mellitus(T2DM).To discover novel and potent DPP-4 inhibitors,three series of compounds were designed and synthesized in this study based on our previously identified novel scaffold of 2-phenyl-3,4-dihydro-2H-benzo[f]*** the designed compounds,41d-1 was the most po tent one with an IC_(50) value of 16.00 nM.

主 题 词：TypeⅡdiabetes Dipeptidyl peptidaseⅣ Inhibitors Molecular docking Structure-activity relationship 

学科分类：1002[医学-临床医学类] 100201[100201] 10[医学] 

核心收录：

D　O　I：10.1002/cjoc.202000342

馆 藏 号：203101428...