文献类型：期刊文献

中文题名：Design, Synthesis and SAR Studies of Novel and Potent Dipeptidyl Peptidase 4 Inhibitors

作者：Na Luo[1];Xiaoyu Fang[1];Mingbo Su[2];Xinwen Zhang[2];Dan Li[3];Honglin Li[1];Shiliang Li[1];Zhenjiang Zhao[1]

机构：[1]Shanghai Key Laboratory of New Drug Design,School of Pharmacy,East China University of Science and Technology,130 Meilong Road,Shanghai 200237,China;[2]State Key Laboratory of Drug Research,Shanghai Institute of Materia Medica,Chinese Academy of Sciences,555 Zhuchongzhi Road,Shanghai 201203,China;[3]Shandong Biopolar Dichang Pharmaceutical Co.,Ltd,RM2306,No.786 Linzi Avenue,Zibo,Shandong 255400,China

年份：2021

卷号：39

期号：1

起止页码：115

中文期刊名：Chinese Journal of Chemistry

外文期刊名：中国化学（英文版）

收录：CSTPCD;;Scopus;CSCD:【CSCD2021_2022】；

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.

语种：英文

中文关键词：TypeⅡdiabetes;Dipeptidyl peptidaseⅣ;Inhibitors;Molecular docking;Structure-activity relationship

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]chromen-3-amine.Among the designed compounds,41d-1 was the most po tent one with an IC_(50) value of 16.00 nM.