Design, synthesis, and antibacterial activity evaluation of tryptanthrin derivatives

IF 2.3 4区医学 Q3 CHEMISTRY, MEDICINAL

Bioorganic & Medicinal Chemistry Letters Pub Date : 2026-03-01 Epub Date: 2025-12-11 DOI:10.1016/j.bmcl.2025.130503

Bing-Yuan Yan , Ran-Qi Feng , Chen Qu , Xu-Wen Li

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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.

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色氨酸衍生物的设计、合成及抗菌活性评价。

设计、合成了一系列色氨酸衍生物，并对其对海洋致病菌副溶血性弧菌的抑菌活性进行了评价。生物活性评价表明，化合物7h和8c对副溶血性弧菌具有较强的抗菌作用，对哺乳动物细胞无细胞毒性。构效关系分析表明，苯基环上的吸电子取代基对提高抗菌活性起着至关重要的作用。此外，化合物7h和8c在浓度分别为8 μg/mL和6 μg/mL时表现出较强的抗生物膜活性，可有效抑制副溶血性弧菌生物膜的形成和成熟。这些结果表明，化合物7h和8c对耐药弧菌具有抑制作用，为色氨酸衍生物作为潜在抗菌剂的应用提供了新的思路。

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来源期刊

Bioorganic & Medicinal Chemistry Letters 医学-医药化学

CiteScore

5.70

自引率

3.70%

发文量

463

审稿时长

27 days

期刊介绍： Bioorganic & Medicinal Chemistry Letters presents preliminary experimental or theoretical research results of outstanding significance and timeliness on all aspects of science at the interface of chemistry and biology and on major advances in drug design and development. The journal publishes articles in the form of communications reporting experimental or theoretical results of special interest, and strives to provide maximum dissemination to a large, international audience.