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ID: ALA1137181

Journal: Bioorg Med Chem Lett

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

Authors: Ahn JH, Kim HM, Jung SH, Kang SK, Kim KR, Rhee SD, Yang SD, Cheon HG, Kim SS.

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.

CiteXplore: 15357972

DOI: 10.1016/j.bmcl.2004.06.046