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A series of novel benzyl-substituted (S)-phenylalanine derivatives were synthesized and evaluated for their dipeptidyl peptidase 4 (DPP-4) inhibitory activity and selectivity. It was found that most synthesized target compounds were potent DPP-4 inhibitors with IC 50 values in 3.79–25.52nM, which were significantly superior to that of the marketed drug sitagliptin. Furthermore, the 4-fluorobenzyl...
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