Citation: Yanye Fan, Jingjing Chen, Bichun Chen, Jinyu Bai, Bowen Yang, Feng Liang, Lijing Fang. Design, synthesis and biological evaluation of Leu₁₀-teixobactin analogues[J]. Chinese Chemical Letters, ;2025, 36(4): 110075. doi: 10.1016/j.cclet.2024.110075 shu

Design, synthesis and biological evaluation of Leu₁₀-teixobactin analogues

Yanye Fan ^{a, b} ,
Jingjing Chen ^{b, e} ,
Bichun Chen ^b ,
Jinyu Bai ^b ,
Bowen Yang ^b ,
Feng Liang ^{a, *,} ,
Lijing Fang ^{b, c, d, *,}

a.
The State Key Laboratory of Refractories and Metallurgy, School of Chemistry and Chemical Engineering, Wuhan University of Science and Technology, Wuhan 430081, China
b.
Guangdong Key Laboratory of Nanomedicine, CAS-HK Joint Lab of Biomaterials, ACS Key Laboratory of Biomedical Imaging Science and System, Institute of Biomedicine and Biotechnology, Shenzhen Institute of Advanced Technology (SIAT), Chinese Academy of Sciences, Shenzhen 518055, China
c.
University of Chinese Academy of Sciences, Beijing 100049, China
d.
Sino-Euro Center of Biomedicine and Health, Shenzhen 518024, China
e.
School of Pharmacy, Lanzhou University, Lanzhou 730000, China

lj.fang@siat.ac.cn

feng_liang@whu.edu.cn

Received Date: 19 March 2024
Revised Date: 16 May 2024
Accepted Date: 30 May 2024
Available Online: 31 May 2024

Figures(3)

Two thioamino acids and four fluorinated amino acids were employed to substitute either partially or entirely the Ile₂, Ser₃, Ile₆, and Ser₇ residues of Leu₁₀-teixobactin to prepare ten analogues and the bioactivity of them was investigated. The SAR studies revealed that Ile₆ was tolerable for both thioamidation and fluoridation, while Ser₇ was identified as the most tolerable site for thioamidation. Analogue 1a demonstrated comparable or slightly improved antibacterial activity, superior protease stability compared to Leu₁₀-teixobactin, while not exhibiting obvious cytotoxicity against mammalian cells.
- Leu₁₀-teixobactin,
- Thioamidation,
- Fluorination,
- Antibacterial activity,
- Protease stability
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Design, synthesis and biological evaluation of Leu10-teixobactin analogues

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通讯作者: 陈斌, bchen63@163.com

Design, synthesis and biological evaluation of Leu₁₀-teixobactin analogues