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Design, synthesis and antimicrobial studies of some polymyxin analogues

The Journal of Antibiotics volume 73, pages 158–166 (2020)Cite this article

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Abstract

To find novel polymycin analogues with high antimicrobial activities and low toxicity, 36 novel polymyxin analogues were synthesized, and in which TZ40-J and TZ40-K were evaluated for their antimicrobial activities using broth microdilution method and for their haemolytic toxicity with sterile sheep blood. Preliminary safety assessments of those two compounds were carried out via the MTT cell viability assay in vitro and acute toxicity assay in vivo. Experimental data demonstrated that TZ40-J and TZ40-K were less toxic and indicate higher activities against Pseudomonas aeruginosa than polymyxin B.

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Acknowledgements

We thank Chitai Tianqing Pharmaceutical Group Co. LTD for acute toxicity assay support.

Funding

This work was supported by the Ministry of Science and Technology of the People’s Republic of China, the national key research and development program (program reference: 2017YFD0501404).

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Authors and Affiliations

  1. Shanghai Duomirui Biotechnology Co., LTD, Shanghai, China

    Hanqing Tang, Jie Ma, Yuanzhen Dong & Jun Feng

  2. China State Institute of Pharmaceutical Industry, Shanghai, China

    You Zhang, Qi Gao & Jun Feng

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  1. Hanqing Tang
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  2. You Zhang
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Correspondence to Jun Feng.

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Tang, H., Zhang, Y., Ma, J. et al. Design, synthesis and antimicrobial studies of some polymyxin analogues. J Antibiot 73, 158–166 (2020). https://doi.org/10.1038/s41429-019-0262-0

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