Natural products as sources of new fungicides (V): Design and synthesis of acetophenone derivatives against phytopathogenic fungi in vitro and in vivo
| Autor: | An-Ling Zhang, Jin-Ming Gao, Wenjia Dan, Thi-Mai-Luong Tuong, Da-Cheng Wang, Ding Li |
|---|---|
| Rok vydání: | 2018 |
| Předmět: |
Clinical Biochemistry
Pharmaceutical Science Microbial Sensitivity Tests 010402 general chemistry 01 natural sciences Biochemistry Microbiology Inhibitory Concentration 50 Structure-Activity Relationship chemistry.chemical_compound Ascomycota In vivo Drug Discovery Magnaporthe grisea Structure–activity relationship Molecular Biology Botrytis cinerea Biological Products Dose-Response Relationship Drug Molecular Structure biology 010405 organic chemistry Chemistry Organic Chemistry Cytospora Acetophenones biology.organism_classification In vitro Fungicides Industrial 0104 chemical sciences Fungicide Magnaporthe Drug Design Molecular Medicine Botrytis Lead compound |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 28:2861-2864 |
| ISSN: | 0960-894X |
| DOI: | 10.1016/j.bmcl.2018.07.031 |
| Popis: | A series of acetophenone derivatives (10a–10i, 11, 12a–12g, 13a–13g, 14a–14d and 15a–15l) were designed, synthesized and evaluated for antifungal activities in vitro and in vivo. The antifungal activities of 53 compounds were tested against several plant pathogens, and their structure–activity relationship was summarized. Compounds 10a–10f displayed better antifungal effects than two reference fungicides. Interestingly, the most potent compound 10d exhibited antifungal properties against Cytospora sp., Botrytis cinerea, Magnaporthe grisea, with IC50 values of 6.0–22.6 µg/mL, especially Cytospora sp. (IC50 = 6.0 µg/mL). In the in vivo antifungal assays, 10d displayed the significant protective efficacy of 55.3% to Botrytis cinerea and 73.1% to Cytospora sp. The findings indicated that 10d may act as a potential pesticide lead compound that merits further investigation. |
| Databáze: | OpenAIRE |
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