2,3,4,5-Tetrahydro-1H-pyrido[2,3-b and e][1,4]diazepines as inhibitors of the bacterial enoyl ACP reductase, FabI |
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| Authors: | Jailall Ramnauth Mathew D. Surman Peter B. Sampson Bryan Forrest Jeff Wilson Emily Freeman David D. Manning Fernando Martin Andras Toro Megan Domagala Donald E. Awrey Elias Bardouniotis Nachum Kaplan Judd Berman Henry W. Pauls |
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| Affiliation: | aAffinium Pharmaceuticals Inc., 1243 Islington Avenue, Suite 600, Toronto, ON, Canada M8X 1Y9;bAMRI, 26 Corporate Circle, PO Box 15098, Albany, NY 12212-5098, USA |
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| Abstract: | In the search for new antibacterial agents, the enzyme FabI has been identified as an attractive target. Employing a structure guided approach, the previously reported ene-amide series of FabI inhibitors were expanded to include 2,3,4,5-tetrahydro-1H-pyrido[2,3-b and e][1,4]diazepines. These novel series incorporate additional H-bonding functions and can be more water soluble than their naphthyridinone progenitors; diazepine 16c is shown to be efficacious in a mouse infection model. |
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| Keywords: | FabI inhibitors 2,3,4,5-Tetrahydro-1H-pyrido [2,3-e][1,4]diazepine Antibacterial Enoyl ACP reductase MRSA Thigh infection model |
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