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Updated: Jan 13, 2026

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
Synthesis and fungicidal evaluation of novel 2-phenyl thiazole derivatives
Xiaofeng Guo1, Han Wang2, Bin Zhao3
1College of Forestry, Central South University of Forestry and Technology, Changsha 410004, PR China; State Key Laboratory of Elemento-Organic Chemistry, College of Chemistry, Nankai University, Tianjin 300071, PR China; State Key Laboratory of Utilization of Woody Oil Resource, Central South University of Forestry and Technology, Changsha 410004, PR China.
Abstract:
Thiazole derivatives possess broad spectrum of biological activities, but only a few thiazole derivatives are developed as commercial fungicides compared to pyrazole and pyridine. In this study, we designed and synthesized 48 novel 2-phenyl thiazole derivatives to evaluate their potential as new fungicides. The results showed that compound 10c displayed excellent in vitro fungicidal activity as compared with positive control thifluzamide against Sclerotinia sclerotiorum, Botrytis cinerea and Rhizoctonia cerealis with corresponding EC50 value of 4.90 vs 4.35, 7.57 vs 10.35 and 7.84 vs 22.12 mg/L, respectively. In addition, compounds 10c exhibited over 80 % of in vivo activity against S. sclerotiorum but lower than thifluzamide (over 90 %) at 10 mg/L. Compound 10c was discovered as novel fungicide leads deserving for further study. The preliminary mode of action study by RNA sequencing indicated that 10c affected the fungi growth by chitin synthase related metabolic reactions.
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