Synthesis and antibacterial properties of beta-diketone acrylate bioisosteres of pseudomonic acid A. |
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| Authors: | I Bennett N J Broom R Cassels J S Elder N D Masson P J O'Hanlon |
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| Affiliation: | SmithKline Beecham Pharmaceuticals, New Frontiers Science Park North, Harlow, Essex, UK. |
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| Abstract: | A series of beta-diketone acrylate bioisosteres 4 of pseudomonic acid A 1 have been synthesized and evaluated for their ability to inhibit bacterial isoleucyl-tRNA synthetase and act as antibacterial agents. A number of analogues have excellent antibacterial activity. Selected examples were shown to afford good blood levels and to be effective in a murine infection model. |
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