کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1364563 981540 2008 5 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Exploration of a fundamental substituent effect of α-ketoheterocycle enzyme inhibitors: Potent and selective inhibitors of fatty acid amide hydrolase
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Exploration of a fundamental substituent effect of α-ketoheterocycle enzyme inhibitors: Potent and selective inhibitors of fatty acid amide hydrolase
چکیده انگلیسی

A series of C4 substituted α-ketooxazoles were examined as inhibitors of the serine hydrolase fatty acid amide hydrolase in efforts that further define and generalize a fundamental substituent effect on enzyme inhibitory potency. Thus, a plot of the Hammett σm versus −log Ki provided a linear correlation (R2 = 0.90) with a slope of 3.37 (ρ = 3.37), that is of a magnitude that indicates that of the electron-withdrawing character of the substituent dominates its effects (a one unit change in σm provides a >1000-fold change in Ki).

A series of C4 substituted α-ketooxazoles were examined as inhibitors of fatty acid amide hydrolase in efforts that further define and generalize a fundamental substituent effect on enzyme inhibitory potency.Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 18, Issue 22, 15 November 2008, Pages 5842–5846
نویسندگان
, , , , ,