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  • Synthesis and DP-IV inhibition of cyano-pyrazoline derivatives as potent anti-diabetic agents.

Synthesis and DP-IV inhibition of cyano-pyrazoline derivatives as potent anti-diabetic agents.

Bioorganic & medicinal chemistry letters (2004-09-11)
Jin Hee Ahn, Hye-Min Kim, Sun Ho Jung, Seung Kyu Kang, Kwang Rok Kim, Sang Dal Rhee, Sung-Don Yang, Hyae Gyeong Cheon, Sung Soo Kim
PMID15357972
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.