Triazolopiperazine-amides as dipeptidyl peptidase IV inhibitors: close analogs of JANUVIA (sitagliptin phosphate).

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Kim D, Kowalchick JE, Edmondson SD, Mastracchio A, Xu J, Eiermann GJ, Leiting B, Wu JK, Pryor KD, Patel RA, He H, Lyons KA, Thornberry NA, Weber AE

Triazolopiperazine-amides as dipeptidyl peptidase IV inhibitors: close analogs of JANUVIA (sitagliptin phosphate).

Bioorg Med Chem Lett. 2007 Jun 15;17(12):3373-7. Epub 2007 Apr 5.

PubMed ID

17434732 [ View in PubMed

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Abstract

A series of beta-aminoamides bearing triazolopiperazines has been prepared and evaluated as potent, selective, orally active dipeptidyl peptidase IV (DPP-4) inhibitors. Efforts at optimization of the beta-aminoamide series, which ultimately led to the discovery of JANUVIA (sitagliptin phosphate, compound 1), are described.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Sitagliptin	Dipeptidyl peptidase 4	IC 50 (nM)	18	N/A	N/A	Details