کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1373095 | 981890 | 2009 | 5 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Design and synthesis of substituted nicotinamides as inhibitors of soluble epoxide hydrolase
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
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چکیده انگلیسی
A series of potent nicotinamide inhibitors of soluble epoxides hydrolase (sEH) is disclosed. This series was designed using structure-based deconstruction and a combination of two HTS hit series, resulting in hybrid analogs that retained the optimal potency from one series, and acceptable in vitro metabolic stability from the other. Structure-guided optimization of these analogs gave rise to nanomolar inhibitors of human sEH that had acceptable plasma exposure to qualify them as probes to determine the in vivo phenotypic consequences of sEH inhibition.
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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 19, Issue 20, 15 October 2009, Pages 5864–5868
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 19, Issue 20, 15 October 2009, Pages 5864–5868
نویسندگان
Steven J. Taylor, Fariba Soleymanzadeh, Anne B. Eldrup, Neil A. Farrow, Ingo Muegge, Alison Kukulka, Alisa K. Kabcenell, Stephane De Lombaert,