2. Academic Validation
  3. Design, synthesis, and antibacterial activity evaluation of tryptanthrin derivatives

Design, synthesis, and antibacterial activity evaluation of tryptanthrin derivatives

  • Bioorg Med Chem Lett. 2026 Mar:132:130503. doi: 10.1016/j.bmcl.2025.130503.
Bing-Yuan Yan 1,  Ran-Qi Feng 2,  Chen Qu 3,  Xu-Wen Li 4
Affiliations

Affiliations

  • 1 School of Pharmacy, Shandong Second Medical University, Weifang 261053, China; Shandong Laboratory of Yantai Drug Discovery, Bohai Rim Advanced Research Institute for Drug Discovery, Yantai 264117, China.
  • 2 Shandong Laboratory of Yantai Drug Discovery, Bohai Rim Advanced Research Institute for Drug Discovery, Yantai 264117, China; University of Chinese Academy of Sciences, Beijing 100049, China.
  • 3 Shandong Laboratory of Yantai Drug Discovery, Bohai Rim Advanced Research Institute for Drug Discovery, Yantai 264117, China.
  • 4 School of Pharmacy, Shandong Second Medical University, Weifang 261053, China; Shandong Laboratory of Yantai Drug Discovery, Bohai Rim Advanced Research Institute for Drug Discovery, Yantai 264117, China; University of Chinese Academy of Sciences, Beijing 100049, China. Electronic address: [email protected].
PMID: 41386540 DOI: 10.1016/j.bmcl.2025.130503
Abstract

A series of tryptanthrin derivatives were designed, synthesized and evaluated for their Antibacterial activity against the marine pathogen Vibrio parahaemolyticus. The bioactivity assessment revealed that compounds 7h and 8c exhibited potent Antibacterial effects against V. parahaemolyticus without cytotoxicity toward mammalian cells. Structure-activity relationship (SAR) analysis indicated that electron-withdrawing substituents on the phenyl ring played a crucial role in enhancing Antibacterial activity. Furthermore, compounds 7h and 8c demonstrated strong antibiofilm activity at concentrations of 8 μg/mL and 6 μg/mL, respectively, effectively inhibiting both biofilm formation and maturation in V. parahaemolyticus. These results demonstrate that compounds 7h and 8c exhibited efficacy against drug-resistant Vibrio strains, providing insight into the application of tryptanthrin derivatives as potential Antibacterial agents.

Keywords

Antibacterial activity; SAR; Tryptanthrin derivatives; Vibrio parahaemolyticus.

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