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Bioorg Med Chem Lett. 1999 Jul 5;9(13):1847-52.

Synthesis and antibacterial properties of beta-diketone acrylate bioisosteres of pseudomonic acid A.

Author information

1
SmithKline Beecham Pharmaceuticals, New Frontiers Science Park North, Harlow, Essex, UK.

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.

PMID:
10406653
DOI:
10.1016/s0960-894x(99)00296-6
[Indexed for MEDLINE]

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