Antibacterial Activity of a Series of N2,N4-Disubstituted Quinazoline-2,4-diamines

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• 作者：Kurt S. Van Horn ; Whittney N. Burda ; Renee Fleeman ; Lindsey N. Shaw ; Roman Manetsch
• 刊名：Journal of Medicinal Chemistry
• 出版年：2014
• 出版时间：April 10, 2014
• 年：2014
• 卷：57
• 期：7
• 页码：3075-3093
• 全文大小：708K
• 年卷期：v.57,no.7(April 10, 2014)
• ISSN：1520-4804

文摘

A series of N²,N⁴-disubstituted quinazoline-2,4-diamines has been synthesized and tested against multidrug resistant Staphylococcus aureus. A structure鈥揳ctivity and structure鈥損roperty relationship study was conducted to identify new hit compounds. This study led to the identification of N²,N⁴-disubstituted quinazoline-2,4-diamines with minimum inhibitory concentrations (MICs) in the low micromolar range in addition to favorable physicochemical properties. Testing of biological activity revealed limited potential for resistance to these agents, low toxicity, and highly effective in vivo activity, even with low dosing regimens. Collectively, these characteristics make this compound series a suitable platform for future development of antibacterial agents.