Author/Authors :
Jin-Hee Ahn، نويسنده , , Hye-Min Kim، نويسنده , , Sun Ho Jung، نويسنده , , Seung Kyu Kang، نويسنده , , Kwang Rok Kim، نويسنده , , Sang Dal Rhee، نويسنده , , Sung-Don Yang، نويسنده , , Hyae Gyeong Cheon، نويسنده , , Sung-Soo Kim، نويسنده ,
Abstract :
A new series of cyano-pyrazoline derivatives with secondary amine at P-2 site was synthesized through achiral and chiral synthetic methods and evaluated for their ability to inhibit dipeptidyl peptidase IV (DP-IV). Compound 5i revealed good in vivo efficacy (ED50: 4.1 mg/kg; in vivo DP-IV inhibition). Also chiral derivative (11b) having (S)-configuration of compound 5i was found to be more potent.
Keywords :
Dipeptidyl peptidase IV , Pyrazoline , DP-IV , Anti-diabeticagent.