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 i...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.展开更多
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.)+3 种基金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.U1501501Shiliang 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.
文摘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.
