Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1374801 | Bioorganic & Medicinal Chemistry Letters | 2008 | 5 Pages |
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 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.
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Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Jin Hee Ahn, Woul Seong Park, Mi Ae Jun, Mi Sik Shin, Seung Kyu Kang, Ki Young Kim, Sang Dal Rhee, Myung Ae Bae, Kwang Rok Kim, Sung Gyu Kim, Sun Young Kim, Sang Kwon Sohn, Nam Sook Kang, Jie Oh Lee, Duck Hyung Lee, Hyae Gyeong Cheon, Sung Soo Kim,