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

…, HM Kim, HM Kwon, SC Huh, S Dal Rhee…

Index: Ahn, Jin Hee; Kim, Jin Ah; Kim, Hye-Min; Kwon, Hyuk-Man; Huh, Sun-Chul; Rhee, Sang Dal; Kim, Kwang Rok; Yang, Sung-Don; Park, Sung-Dae; Lee, Jae Mok; Kim, Sung Soo; Cheon, Hyae Gyeong Bioorganic and Medicinal Chemistry Letters, 2005 , vol. 15, # 5 p. 1337 - 1340

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Citation Number: 32

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 IC 50 value of 1.56 μM and ED 50 value of 80 mg/kg (in vivo DP-IV inhibition; po). ... Recently, we have reported the synthesis and biological evaluation of a new series of cyano-pyrazoline derivatives with the secondary amine at P-2 position 6 (Fig. 1). ... This compound (Fig. 1) showed a ...