1. Triaminotriazine DNA helicase inhibitors with antibacterial activity
- Author
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McKay, Geoffrey A., Reddy, Ranga, Arhin, Francis, Belley, Adam, Lehoux, Dario, Moeck, Greg, Sarmiento, Ingrid, Parr, Thomas R., Gros, Philippe, Pelletier, Jerry, and Far, Adel Rafai
- Subjects
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DNA helicases , *PSEUDOMONAS aeruginosa , *ANTIBACTERIAL agents , *ANTINEOPLASTIC antibiotics - Abstract
Abstract: Screening of a chemical library in a DNA helicase assay involving the Pseudomonas aeruginosa DnaB helicase provided a triaminotriazine inhibitor with good antibacterial activity but associated cytotoxicity toward mammalian cells. Synthesis of analogs provided a few inhibitors that retained antibacterial activity and demonstrated a significant reduction in cytotoxicity. The impact of serum and initial investigations toward a mode of action highlight several features of this class of compounds as antibacterials. [Copyright &y& Elsevier]
- Published
- 2006
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