Anti-Virulence Strategy of Novel Dehydroabietic Acid Derivatives: Design, Synthesis, and Antibacterial Evaluation
Anti-virulence strategies are attractive and interesting strategies for controlling bacterial diseases because virulence factors are fundamental to the infection process of numerous serious phytopathogenics. To extend the novel anti-virulence agents, a series of dehydroabietic acid (DAA) derivatives...
Main Authors: | , , , , , , , , , |
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Format: | Article |
Language: | English |
Published: |
MDPI AG
2023-02-01
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Series: | International Journal of Molecular Sciences |
Subjects: | |
Online Access: | https://www.mdpi.com/1422-0067/24/3/2897 |
Summary: | Anti-virulence strategies are attractive and interesting strategies for controlling bacterial diseases because virulence factors are fundamental to the infection process of numerous serious phytopathogenics. To extend the novel anti-virulence agents, a series of dehydroabietic acid (DAA) derivatives decorated with amino alcohol unit were semi-synthesized based on structural modification of the renewable natural DAA and evaluated for their antibacterial activity against <i>Xanthomonas oryzae</i> pv<i>. oryzae</i> (<i>Xoo</i>), <i>Xanthomonas axonopodis</i> pv. <i>citri</i> (<i>Xac</i>), and <i>Pseudomonas syringae</i> pv. <i>actinidiae</i> (<i>Psa</i>). Compound <b>2b</b> showed the most promising antibacterial activity against <i>Xoo</i> with an EC<sub>50</sub> of 2.7 μg mL<sup>−1</sup>. Furthermore, compound <b>2b</b> demonstrated remarkable control effectiveness against bacterial leaf blight (BLB) in rice, with values of 48.6% and 61.4% for curative and protective activities. In addition, antibacterial behavior suggested that compound <b>2b</b> could suppress various virulence factors, including EPS, biofilm, swimming motility, and flagella. Therefore, the current study provided promising lead compounds for novel bactericides discovery by inhibiting bacterial virulence factors. |
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ISSN: | 1661-6596 1422-0067 |