کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1373599 | 981903 | 2007 | 7 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Synthesis, biological evaluation and structural determination of β-aminoacyl-containing cyclic hydrazine derivatives as dipeptidyl peptidase IV (DPP-IV) inhibitors
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
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چکیده انگلیسی
Inhibitors of dipeptidyl peptidase IV (DPP-IV) have been shown to be effective treatments for type 2 diabetes. A series of β-aminoacyl-containing cyclic hydrazine derivatives were synthesized and evaluated as DPP-IV inhibitors. One member of this series, (R)-3-amino-1-(2-benzoyl-1,2-diazepan-1-yl)-4-(2,4,5-trifluorophenyl)butan-1-one (10f), showed potent in vitro activity, good selectivity and in vivo efficacy in mouse models. Also, the binding mode of compound 10f was determined by X-ray crystallography.
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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 17, Issue 9, 1 May 2007, Pages 2622–2628
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 17, Issue 9, 1 May 2007, Pages 2622–2628
نویسندگان
Jin Hee Ahn, Mi Sik Shin, Mi Ae Jun, Sun Ho Jung, Seung Kyu Kang, Kwang Rok Kim, Sang Dal Rhee, Nam Sook Kang, Sun Young Kim, Sang-Kwon Sohn, Sung Gyu Kim, Mi Sun Jin, Jie Oh Lee, Hyae Gyeong Cheon, Sung Soo Kim,