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- Title
Design, Synthesis and Fungicidal Activity of N-(5-Phenyl-1,3,4-Thiadiazol-2-yl)-N-((1-Phenyl-1 H -1,2,3-Triazol-4-yl) Methyl) Benzamide Derivatives.
- Authors
Kong, Ziyi; Zhang, Xinyu; Bian, Ming; Fu, Danni
- Abstract
Objective: Plant pathogens are serious hazards to agricultural production, but existing drugs have problems such as increased resistance of pathogenic bacteria and environmental pollution, and there is a need to find high-efficiency, low-toxicity fungicides with novel chemical structures. Methods: 5-phenyl-1,3,4-thiadiazol-2-amine was used as the starting material, and 20 new thiadiazole-linked compounds were designed and synthesized. Their in vitro inhibitory activities against plant pathogenic fungi were tested using a mycelium growth inhibition assay, and the relationship between the antifungal activity of the target compounds and their molecular structures was preliminarily discussed. Results: Bioassay results revealed that most of the title compounds exhibited excellent in vitro fungicidal activity, in which compound D16 showed the highest activity against Rhizoctonia solani (EC50 = 0.0028 μmol·L−1), D12 against Botrytis cinerea (EC50 = 0.0024 μmol·L−1), and D5 against Stemphylium lycopersici and Curvularia lunata (EC50 = 0.0105 μmol·L−1, 0.005 μmol·L−1). The structure activity relationship (SAR) was also discussed and the results are of great significance for the structural optimization and development of more effective thiadiazole antibacterial compounds. Conclusion: The results of this study are important for structural optimization and development of more potent thiadiazole antimicrobial compounds.
- Subjects
STRUCTURE-activity relationships; PHYTOPATHOGENIC microorganisms; RHIZOCTONIA solani; PHYTOPATHOGENIC fungi; STRUCTURAL optimization
- Publication
Natural Product Communications, 2024, Vol 19, Issue 12, p1
- ISSN
1934-578X
- Publication type
Academic Journal
- DOI
10.1177/1934578X241304621