1006706-47-3Relevant academic research and scientific papers
Synthesis and biological evaluation of homopiperazine derivatives with β-aminoacyl group as dipeptidyl peptidase IV inhibitors
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
supporting information; experimental part, p. 6525 - 6529 (2009/09/06)
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 prototype for further derivatization. Based on its X-ray co-crystal structure with human DPP-IV, we identified compounds 7s and 7t which showed good in vitro activity, no CYP inhibition, and good selectivity.
