Article ID Journal Published Year Pages File Type
10593082 Bioorganic & Medicinal Chemistry Letters 2012 5 Pages PDF
Abstract
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.
Related Topics
Physical Sciences and Engineering Chemistry Organic Chemistry
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