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Synergism of Fused Bicyclic 2-Aminothiazolyl compounds with polymyxin B against Klebsiella pneumonia

Abstract

A series of fused bicyclic 2-aminothiazolyl compounds were synthesized and evaluated for their synergistic effects with polymyxin B (PB) against Klebsiella pneumonia (SIPI-KPN-1712). Some of the synthesized compounds exhibited synergistical activity. When 4 μg/ml compound B1 was combined with PB, it showed potent antibacterial activity, achieving 64-fold reduction for the MIC of PB. Furthermore, compound B1 showed prominent synergistic efficacy in both concentration gradient and time–kill curves in vitro. In addition, B1 combined with PB also exhibited synergistic and partial synergistic against E. coli (ATCC25922 and its clinical isolates), Acinetobacter baumanii (ATCC19606 and its clinical isolates), and Pseudomonas aeruginosa (Pae-1399).

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Publication details

The article was received on 14 Jul 2017, accepted on 14 Sep 2017 and first published on 14 Sep 2017


Article type: Research Article
DOI: 10.1039/C7MD00354D
Citation: Med. Chem. Commun., 2017, Accepted Manuscript
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    Synergism of Fused Bicyclic 2-Aminothiazolyl compounds with polymyxin B against Klebsiella pneumonia

    R. wang, S. hou, X. Dong, D. Chen, L. Shao, L. qian, Z. Li and X. Xu, Med. Chem. Commun., 2017, Accepted Manuscript , DOI: 10.1039/C7MD00354D

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