Related Experiment Video
Updated: Feb 20, 2026

Synthesis of Masarimycin, a Small Molecule Inhibitor of Gram-Positive Bacterial Growth
Published on: January 7, 2022
Chiral Mandelic Acid Derivatives as Inhibitors Targeting the Type III Secretion System of Xanthomonas citri Subsp.
Jinyuan Wei1, Xin Wang1,2, Jiaxin Xian1
1State Key Laboratory of Green Pesticide, Integrative Microbiology Research Center, Guangdong Provincial Key Laboratory of Microbial Signals and Disease Control, College of Plant Protection, South China Agricultural University, Guangzhou 510642, China.
Abstract:
Xanthomonas citri subsp. citri (Xcc), the pathogen responsible for citrus canker, causes major economic damage worldwide. The type III secretion system (T3SS) is essential for Xcc pathogenicity. Here, 39 chiral 1,3,4-oxadiazole sulfide derivatives of mandelic acid were synthesized, with 17 compounds exhibiting significant inhibitory activity (>70% inhibition) against the T3SS of Xcc jx-6 at 40 μg/mL. Among these, the R-configuration WR4 significantly suppressed the symptoms of citrus canker in an in vivo bioassay, whereas neither the S-configuration WS4 nor the racemic mixture WRS4 showed inhibitory effects. Mechanistically, WR4 suppressed T3SS gene transcription and Hpa1 protein secretion, and counteracted pathogen-induced suppression of host immunity, without affecting other virulence factors. From an environmental safety perspective, WR4 exhibited low toxicity against nontarget organisms, including earthworms, silkworms, and zebrafish. These findings reveal the potential of the R-configuration derivatives as sustainable T3SS inhibitors.
More Related Videos
08:20Systematic Approach to Identify Novel Antimicrobial and Antibiofilm Molecules from Plants' Extracts and Fractions to Prevent Dental Caries
Published on: March 31, 2021
03:29Author Spotlight: Advancing Therapeutics to Treat Vibriosis in Humans and Aquatic Organisms
Published on: May 31, 2024
Related Concept Videos
Indirect-Acting Cholinergic Agonists: Chemistry and Structure-Activity Relationship
Reversible inhibitors display short to medium durations of action. Short-acting agents include simple alcohols with...
Cholinergic Antagonists: Chemistry and Structure-Activity Relationship
Direct-Acting Cholinergic Agonists: Chemistry and Structure-Activity Relationship
The direct-acting...
Molecules with Multiple Chiral Centers
Indirect-Acting Cholinergic Agonists: Mechanism of Action
Reversible inhibitors like edrophonium bind to a specific part of the enzyme called the anionic catalytic site. They form noncovalent bonds, which means they are not strongly attached to the enzyme. This creates a temporary and less stable enzyme–inhibitor complex,...
Cholinergic Antagonists: Pharmacokinetics