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Optimization of 1,4-diazepan-2-one containing dipeptidyl peptidase IV inhibitors for the treatment of type 2 diabetes.

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 IC(50)=8.0 nM) and 3R,6R-dimethyl-1,4-diazepan-2-one derivative 14a (DPP-4 IC(50)=9.7 nM).

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Liang GB,Qian X,Feng D,Biftu T,Eiermann G,He H,Leiting B,Lyons K,Petrov A,Sinha-Roy R,Zhang B,Wu J,Zhang X,Thornberry NA,Weber AE

doi

10.1016/j.bmcl.2007.01.039

subject

Has Abstract

pub_date

2007-04-01 00:00:00

pages

1903-7

issue

7

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(07)00090-X

journal_volume

17

pub_type

杂志文章

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