Title of article
Optimization of 1,4-diazepan-2-one containing dipeptidyl peptidase IV inhibitors for the treatment of type 2 diabetes
Author/Authors
Gui-Bai Liang، نويسنده , , Xiaoxia Qian، نويسنده , , Dennis Feng، نويسنده , , Tesfaye Biftu، نويسنده , , George Eiermann، نويسنده , , Huaibing He، نويسنده , , Barbara Leiting، نويسنده , , Kathy Lyons، نويسنده , , Aleksandr Petrov، نويسنده , , Ranabir Sinha-Roy، نويسنده , , Bei Zhang، نويسنده , , Joseph Wu، نويسنده , , Xiaoping Zhang، نويسنده , , Nancy A. Thornberry، نويسنده , , Ann E. Weber، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2007
Pages
5
From page
1903
To page
1907
Abstract
Following the discovery of N-acyl-1,4-diazepan-2-one as a novel pharmacophore for potent and selective DPP-4 inhibitors, optimization of this new lead with different substitution on the seven-membered ring resulted in several highly potent and selective, orally bioavailable, and efficacious DPP-4 inhibitors, such as 3R-methyl-1-cyclopropyl-1,4-diazepan-2-one derivative 9i (DPP-4 IC50 = 8.0 nM) and 3R,6R-dimethyl-1,4-diazepan-2-one derivative 14a (DPP-4 IC50 = 9.7 nM).
Keywords
Type 2 diabetes , DPP-IV inhibitors , 1 , 4-Diazepan-2-one
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2007
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
797955
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