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RSS FeedsMarine Drugs, Vol. 20, Pages 740: Discovery of Novel Pimprinine and Streptochlorin Derivatives as Potential Antifungal Agents (Marine Drugs)

 
 

25 november 2022 14:45:28

 
Marine Drugs, Vol. 20, Pages 740: Discovery of Novel Pimprinine and Streptochlorin Derivatives as Potential Antifungal Agents (Marine Drugs)
 


Pimprinine and streptochlorin are indole alkaloids derived from marine or soil microorganisms. In our previous study, they were promising lead compounds due to their potent bioactivity in preventing many phytopathogens, but further structural modifications are required to improve their antifungal activity. In this study, pimprinine and streptochlorin were used as parent structures with the combination strategy of their structural features. Three series of target compounds were designed and synthesized. Subsequent evaluation for antifungal activity against six common phytopathogenic fungi showed that some of thee compounds possessed excellent effects, and this is highlighted by compounds 4a and 5a, displaying 99.9% growth inhibition against Gibberella zeae and Alternaria Leaf Spot under 50 μg/mL, respectively. EC50 values indicated that compounds 4a, 5a, 8c, and 8d were even more active than Azoxystrobin and Boscalid. SAR analysis revealed the relationship between 5-(3′-indolyl)oxazole scaffold and antifungal activity, which provides useful insight into the development of new target molecules. Molecular docking models indicate that compound 4a binds with leucyl-tRNA synthetase in a similar mode as AN2690, offering a perspective on the mode of action for the study of its antifungal activity. These results suggest that compounds 4a and 5a could be regarded as novel and promising antifungal agents against phytopathogens due to their valuable potency.


 
47 viewsCategory: Biochemistry, Molecular Biology, Pharmacology
 
Marine Drugs, Vol. 20, Pages 739: Gelatin from Saithe (Pollachius virens) Skin: Biochemical Characterization and Oxidative Stability in O/W Emulsions (Marine Drugs)
Marine Drugs, Vol. 20, Pages 741: κ- and λ-Carrageenans from Marine Alga Сhondrus armatus Exhibit Anticancer In Vitro Activity in Human Gastrointestinal Cancers Models (Marine Drugs)
 
 
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