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Synthesis and Biological Evaluation of Xanthine Derivatives on Dipeptidyl Peptidase 4

2013; Pharmaceutical Society of Japan; Volume: 61; Issue: 4 Linguagem: Inglês

10.1248/cpb.c12-01046

1347-5223

Kuaile Lin, Zhengyan Cai, Fei Wang, Wei Zhang, Weicheng Zhou,

Signaling Pathways in Disease

A series of xanthine derivatives in which a methylene was inserted at position 8 of xanthine scaffold was synthesized and evaluated as inhibitors of dipeptidyl peptidase 4 (DPP-4) for the treatment of type 2 diabetes. As the results of structure–activity relationship (SAR) study of the series, the compounds with 4-methyl-quinazoline-2-yl-methyl group at N-1 position and 2-aminoethylaminomethyl group gave better activities. Compounds H4 and H9 showed good DPP-4 inhibition and more than 100-fold selectivity over DPP-7 and DPP-8.