کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1393399 | 1501209 | 2008 | 14 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Synthesis and biological evaluation of pyrazoline analogues with β-amino acyl group as dipeptidyl peptidase IV inhibitors
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
A series of pyrazoline derivatives with β-amino acyl group were synthesized and evaluated for their ability to inhibit dipeptidyl peptidase IV. Several pyrazoline derivatives exhibited submicromolar inhibitory activities against DPP-IV. X-ray co-crystal structure of initial hit compound 1h was determined. Among this series, carboxylic acid substituted pyrazoline derivative 2u was the most active and greatly decreased the inhibitory activity toward CYP3A4 enzyme.
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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: European Journal of Medicinal Chemistry - Volume 43, Issue 9, September 2008, Pages 1889–1902
Journal: European Journal of Medicinal Chemistry - Volume 43, Issue 9, September 2008, Pages 1889–1902
نویسندگان
Mi Ae Jun, Woul Seong Park, Seung Kyu Kang, Ki Young Kim, Kwang Rok Kim, Sang Dal Rhee, Myung Ae Bae, Nam Sook Kang, Sang-Kwon Sohn, Sung Gyu Kim, Jie Oh Lee, Duck Hyung Lee, Hyae Gyeong Cheon, Sung Soo Kim, Jin Hee Ahn,