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The dihydrochloride of 1-[[5-(aminomethyl)-2-methyl-4-(4-methylphenyl)-6-(2-methylpropyl) pyridin-3-yl]acetyl]-L-prolinamide (41) was identified as showing selective inhibitory activity against DPP-4, capable of interacting with the guanidino group of Arg125 in a bidentate manner (Figure 6)

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