کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1374801 | 981924 | 2008 | 5 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Synthesis and biological evaluation of homopiperazine derivatives with β-aminoacyl group as dipeptidyl peptidase IV inhibitors
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
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چکیده انگلیسی
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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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 18, Issue 24, 15 December 2008, Pages 6525–6529
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 18, Issue 24, 15 December 2008, Pages 6525–6529
نویسندگان
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,