Synthesis and antibacterial properties of β-diketone acrylate bioisosteres of pseudomonic acid A
摘要:
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. (C) 1999 Elsevier Science Ltd. All rights reserved.
Synthesis and antibacterial properties of β-diketone acrylate bioisosteres of pseudomonic acid A
摘要:
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. (C) 1999 Elsevier Science Ltd. All rights reserved.