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Synthesis and evaluation of pyrazolidine derivatives as dipeptidyl peptidase IV (DP-IV) inhibitors

Jin Hee Ahn,Jin Ah Kim,Hye-Min Kim,Hyuk-Man Kwon,Sun-Chul Huh,Sang Dal Rhee,Kwang Rok Kim,Sung-Don Yang,Sung-Dae Park,Jae Mok Lee,Sung Soo Kim,Hyae Gyeong Cheon

Bioorganic & Medicinal Chemistry Letters（2005）

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Abstract
A new series of pyrazolidine derivatives was synthesized and evaluated for their ability to inhibit dipeptidyl peptidase IV (DP-IV). Compound 9i was the most active in this series, exhibited IC50 value of 1.56μM and ED50 value of 80mg/kg (in vivo DP-IV inhibition; po).
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Key words
Dipeptidyl peptidase IV,DP-IV,Pyrazolidine,Anti-diabetic agent
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