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Novel trans-2-aryl-cyclopropylamine analogues as potent and selective dipeptidyl peptidase IV inhibitors.

Abstract：

:A series of trans-2-aryl-cyclopropylamine derived compounds were synthesized and evaluated their biological activities against DPP-IV. The structure-activity relationships (SAR) led to the discovery of novel series of DPP-IV inhibitors, having IC(50) values of <100 nM with excellent selectivity over the closely related enzymes, DPP8, DPP-II and FAP. The studies identified a potent and selective DPP-IV inhibitor 24b, which exhibited the ability to both significantly inhibit plasma DPP-IV activity in rats and improve glucose tolerance in lean mice and diet induced obese mice.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Tsai TY,Hsu T,Chen CT,Cheng JH,Yeh TK,Chen X,Huang CY,Chang CN,Yeh KC,Hsieh SH,Chien CH,Chang YW,Huang CH,Huang YW,Huang CL,Wu SH,Wang MH,Lu CT,Chao YS,Jiaang WT

doi

10.1016/j.bmc.2009.02.020

subject

Has Abstract

pub_date

2009-03-15 00:00:00

pages

2388-99

issue

6

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(09)00135-7

journal_volume

17

pub_type

杂志文章

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