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(3R)-4-[(3R)-3-Amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-(2,2,2-trifluoroethyl)-1,4-diazepan-2-one, a Selective Dipeptidyl Peptidase IV Inhibitor for the Treatment of Type 2 Diabetes

(3R)-4-[(3R)-3-Amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-(2,2,2-trifluoroethyl)-1,4-diazepan-2-one, a Selective Dipeptidyl Peptidase IV Inhibitor for the Treatment of Type 2 Diabetes

Tesfaye Biftu, Dennis Feng, Xiaoxia Qian, Gui-Bai Liang, Gerard Kieczykowski, George Eiermann, Huaibing He, Barbara Leiting, Kathy Lyons, Aleksandr Petrov, Ranabir Sinha-Roy, Bei Zhang, Giovanna Scapin, etc.

Bioorg Med Chem Lett. 2007 Jan 1;17(1):49-52.

PMID: 17055272

Abstract:

Replacement of the triazolopiperazine ring of sitagliptin (DPP-4 IC(50)=18nM) with 3-(2,2,2-trifluoroethyl)-1,4-diazepan-2-one gave dipeptidyl peptidase IV (DPP-4) inhibitor 1 which is potent (DPP-4 IC(50)=2.6nM), selective, and efficacious in an oral glucose tolerance test in mice. It was selected for extensive preclinical development as a potential back-up candidate to sitagliptin.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP22753806	2-[N-(2,2,2-Trifluoroethyl)amino]-5-chlorobenzophenone		22753-80-6	Price

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