Design, synthesis and antibacterial activity of 3-methylenepyrrolidine formyl hydroxyamino derivatives as novel peptide deformylase inhibitors |
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| Authors: | Shi Wei Ma Haikun Duan Yuejiao Aubart Kelly Fang Yuhong Zonis Rimma Yang Liping Hu Wenhao |
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| Institution: | a Institute of Drug Discovery and Development, and Department of Chemistry, East China Normal University, Shanghai 200062, China
b Antibacterial DPU, GlaxoSmithKline, Collegeville, PA 19426, USA |
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| Abstract: | 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 P3′ positions, and most of these derivatives exhibit better in vitro antibacterial activity than existing drugs against drug-resistant clinical isolates including MRSA, PRSP, and Haemophilus influenzae. |
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| Keywords: | PDF inhibitor Antibiotics Drug-resistant bacteria Pyrrolidine derivatives |
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