کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
10593082 981804 2012 5 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Discovery of bacterial NAD+-dependent DNA ligase inhibitors: Improvements in clearance of adenosine series
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Discovery of bacterial NAD+-dependent DNA ligase inhibitors: Improvements in clearance of adenosine series
چکیده انگلیسی
Optimization of clearance of adenosine inhibitors of bacterial NAD+-dependent DNA ligase is discussed. To reduce Cytochrome P-450-mediated metabolic clearance, many strategies were explored; however, most modifications resulted in compounds with reduced antibacterial activity and/or unchanged total clearance. The alkyl side chains of the 2-cycloalkoxyadenosines were fluorinated, and compounds with moderate antibacterial activity and favorable pharmacokinetic properties in rat and dog were identified.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 22, Issue 1, 1 January 2012, Pages 85-89
نویسندگان
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