Synthesis and DP-IV inhibition of cyano-pyrazoline derivatives as potent anti-diabetic agents
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: 4.1mg/kg; in vivo DP-IV inhibition). Also chiral derivative (11b) having (S)-configuration of compound 5i was found to be more potent.
Ahn, Jin Hee,Kim, Hye-Min,Jung, Sun Ho,Kang, Seung Kyu,Kim, Kwang Rok,Rhee, Sang Dal,Yang, Sung-Don,Cheon, Hyae Gyeong,Kim, Sung Soo
p. 4461 - 4465
(2007/10/03)
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