Synthesis and Antibacterial Properties of β-Diketone Acrylate Bioisosteres of Pseudomonic Acid A.

Abstract A series of β-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 show to afford good blood levels and to be effective in a murine infection model.