Potent non-nitrile dipeptidic dipeptidyl peptidase IV inhibitors.

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Simpkins LM, Bolton S, Pi Z, Sutton JC, Kwon C, Zhao G, Magnin DR, Augeri DJ, Gungor T, Rotella DP, Sun Z, Liu Y, Slusarchyk WS, Marcinkeviciene J, Robertson JG, Wang A, Robl JA, Atwal KS, Zahler RL, Parker RA, Kirby MS, Hamann LG

Potent non-nitrile dipeptidic dipeptidyl peptidase IV inhibitors.

Bioorg Med Chem Lett. 2007 Dec 1;17(23):6476-80. Epub 2007 Oct 1.

PubMed ID

17937986 [ View in PubMed

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Abstract

The synthesis and structure-activity relationships of novel dipeptidyl peptidase IV inhibitors replacing the classical cyanopyrrolidine P1 group with other small nitrogen heterocycles are described. A unique potency enhancement was achieved with beta-branched natural and unnatural amino acids, particularly adamantylglycines, linked to a (2S,3R)-2,3-methanopyrrolidine based scaffold.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Saxagliptin	Dipeptidyl peptidase 4	Ki (nM)	0.6	N/A	N/A	Details