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

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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

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

Bioorg Med Chem. 2009 Mar 15;17(6):2388-99. doi: 10.1016/j.bmc.2009.02.020. Epub 2009 Feb 20.

PubMed ID

19261480 [ View in PubMed

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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.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Sitagliptin	Dipeptidyl peptidase 4	IC 50 (nM)	30	N/A	N/A	Details
Vildagliptin	Dipeptidyl peptidase 4	IC 50 (nM)	51	N/A	N/A	Details