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Spiro-naphthyridinone piperidines as inhibitors of S. aureus and E. coli enoyl-ACP reductase (FabI) |
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| Authors: | Peter B Sampson Christine Picard Sean Handerson Teresa E McGrath Megan Domagala Andrew Leeson Vladimir Romanov Donald E Awrey Dhushy Thambipillai Elias Bardouniotis Nachum Kaplan Judd M Berman Henry W Pauls |
| Institution: | aAffinium Pharmaceuticals Inc. 1243 Islington Ave., Suite 600, Toronto, Ontario, Canada M8X 1Y9 |
| Abstract: | Spiropiperidine naphthyridinone inhibitors of Staphylococcus aureus and Escherichia coli FabI have been prepared. Compounds 14a and 14c were identified as having sub-nanomolar E. coli FabI activity and are among the most potent FabI inhibitors yet described. The structural model of 14a bound to E. coli FabI is shown. |
| Keywords: | Enoyl-ACP reductase Naphthyridinone |
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