2. Academic Validation
  3. Synthesis and biofilm inhibitory activity of cyclic dinucleotide analogues prepared with macrocyclic ribose-phosphate skeleton

Synthesis and biofilm inhibitory activity of cyclic dinucleotide analogues prepared with macrocyclic ribose-phosphate skeleton

  • Bioorg Med Chem Lett. 2025 Apr 15:119:130107. doi: 10.1016/j.bmcl.2025.130107.
Di Xie 1,  Lingyun Xu 1,  Shuwei Yuan 1,  Jiayin Yan 1,  Peng Zhou 1,  Wenpei Dong 1,  Jinliang Ma 2,  Changpo Chen 3
Affiliations

Affiliations

  • 1 Collaborative Innovation Center of Henan Province for Green Manufacturing of Fine Chemicals, Key Laboratory of Green Chemical Media and Reactions, Ministry of Education, Henan Key Laboratory of Organic Functional Molecule and Drug Innovation, School of Chemistry and Chemical Engineering, Henan Normal University, Xinxiang, Henan 453007, PR China.
  • 2 Collaborative Innovation Center of Henan Province for Green Manufacturing of Fine Chemicals, Key Laboratory of Green Chemical Media and Reactions, Ministry of Education, Henan Key Laboratory of Organic Functional Molecule and Drug Innovation, School of Chemistry and Chemical Engineering, Henan Normal University, Xinxiang, Henan 453007, PR China. Electronic address: majinliang@htu.edu.cn.
  • 3 Collaborative Innovation Center of Henan Province for Green Manufacturing of Fine Chemicals, Key Laboratory of Green Chemical Media and Reactions, Ministry of Education, Henan Key Laboratory of Organic Functional Molecule and Drug Innovation, School of Chemistry and Chemical Engineering, Henan Normal University, Xinxiang, Henan 453007, PR China. Electronic address: chenchangpo@htu.edu.cn.
PMID: 39828003 DOI: 10.1016/j.bmcl.2025.130107
Abstract

Cyclic diguanosine monophosphate (c-di-GMP) is the key second messenger regulating Bacterial biofilm formation related genes. Several c-di-GMP analogues have demonstrated biofilm inhibition activity. In this study, ribose-phosphate macrocyclic skeleton containing 1'-azido groups was constructed, and CDN analogues were prepared via Click Chemistry. The biofilm formation inhibition activity of the analogues was evaluated, and compound 17 illustrated better activity than c-di-GMP. This high-throughput strategy could be extended to synthesize cyclic analogues for biological research and immunotherapeutic development.

Keywords

Biofilm inhibition; Macrocyclic ribose-phosphate skeleton; Triazole; c-di-GMP.

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