- Synthesis, antibacterial activity, and biological evaluation of formyl hydroxyamino derivatives as novel potent peptide deformylase inhibitors against drug-resistant bacteria
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Peptide deformylase (PDF) has been identified as a promising target for novel antibacterial agents. In this study, a series of novel formyl hydroxyamino derivatives were designed and synthesized as PDF inhibitors and their antibacterial activities were evaluated. Among the potent PDF inhibitors (1o, 1q, 1o′, 1q′, and 1x), in vivo studies showed that compound 1q possesses mild toxicity, a good pharmacokinetic profile and protective effects. The good in vivo efficacy and low toxicity suggest that this class of compounds has potential for development and use in future antibacterial drugs.
- Yang, Shouning,Shi, Wei,Xing, Dong,Zhao, Zheng,Lv, Fengping,Yang, Liping,Yang, Yushe,Hu, Wenhao
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p. 133 - 152
(2014/10/15)
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- Design, synthesis and antibacterial activity of 3-methylenepyrrolidine formyl hydroxyamino derivatives as novel peptide deformylase inhibitors
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The synthesis and antibacterial activity of 3-methylenepyrrolidine formyl hydroxyamino derivatives are reported. The antibacterial activities of these derivatives were evaluated to discover SAR at P1′ and P 3′ positions, and most of
- Shi, Wei,Ma, Haikun,Duan, Yuejiao,Aubart, Kelly,Fang, Yuhong,Zonis, Rimma,Yang, Liping,Hu, Wenhao
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p. 1060 - 1063
(2011/03/21)
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