Triaminotriazine DNA helicase inhibitors with antibacterial activity |
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Authors: | McKay Geoffrey A Reddy Ranga Arhin Francis Belley Adam Lehoux Dario Moeck Greg Sarmiento Ingrid Parr Thomas R Gros Philippe Pelletier Jerry Far Adel Rafai |
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Institution: | Targanta Therapeutics Inc., 7170 Frederick Banting, 2nd Floor, St. Laurent, Québec, Canada H4S 2A1. |
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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. |
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