Synthesis and biological evaluation of pyrazoline analogues with beta-amino acyl group as dipeptidyl peptidase IV inhibitors.

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Jun MA, Park WS, Kang SK, Kim KY, Kim KR, Rhee SD, Bae MA, Kang NS, Sohn SK, Kim SG, Lee JO, Lee DH, Cheon HG, Kim SS, Ahn JH

Synthesis and biological evaluation of pyrazoline analogues with beta-amino acyl group as dipeptidyl peptidase IV inhibitors.

Eur J Med Chem. 2008 Sep;43(9):1889-902. doi: 10.1016/j.ejmech.2007.11.029. Epub 2007 Dec 14.

PubMed ID
18243422 [ View in PubMed
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Abstract

A series of pyrazoline derivatives with beta-amino acyl group were synthesized and evaluated for their ability to inhibit dipeptidyl peptidase IV. Several pyrazoline derivatives exhibited submicromolar inhibitory activities against DPP-IV. X-ray co-crystal structure of initial hit compound 1h was determined. Among this series, carboxylic acid substituted pyrazoline derivative 2u was the most active and greatly decreased the inhibitory activity toward CYP3A4 enzyme.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
SitagliptinDipeptidyl peptidase 4IC 50 (nM)110N/AN/ADetails