Synthesis and biological evaluation of homopiperazine derivatives with β-aminoacyl group as dipeptidyl peptidase IV inhibitors

…, KY Kim, S Dal Rhee, MA Bae, KR Kim, SG Kim…

Index: Ahn, Jin Hee; Park, Woul Seong; Jun, Mi Ae; Shin, Mi Sik; Kang, Seung Kyu; Kim, Ki Young; Rhee, Sang Dal; Bae, Myung Ae; Kim, Kwang Rok; Kim, Sung Gyu; Kim, Sun Young; Sohn, Sang Kwon; Kang, Nam Sook; Lee, Jie Oh; Lee, Duck Hyung; Cheon, Hyae Gyeong; Kim, Sung Soo Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 24 p. 6525 - 6529

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Citation Number: 16

Abstract

Compounds with homopiperazine skeleton are designed to find a potent DPP-IV inhibitor without inhibiting CYP. Thus a series of β-aminoacyl-containing homopiperazine derivatives was synthesized and evaluated. Compounds with acid moiety were found to be potent inhibitors of DPP-IV without inhibiting CYP 3A4. More specifically, compound 7m showed nanomolar activity with no inhibition towards five subtypes of CYPs, was considered as a ...