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Published on: February 14, 2018
Core Emulating Optimization of Mycoleptodiscin A for Synthetically Tractable Antifungal Leads
Nvdan Hu1,2, Shengxin Sun1, Xian Ming1
1State Key Laboratory of Green Pesticide, Center for R&D of Fine Chemicals of Guizhou University, Guiyang 550025, China.
Journal of Agricultural and Food Chemistry
|May 18, 2026
Summary
Researchers optimized mycoleptodiscin A to create novel antifungal compounds. Several drimane heterocycles showed significant potential against plant pathogens like *R. solani* and *S. sclerotiorum*.
Area of Science:
- Medicinal Chemistry
- Agrochemicals
- Organic Synthesis
Background:
- Mycoleptodiscin A serves as a basis for developing new antifungal agents.
- Optimization is needed to create synthetically feasible and potent antifungal compounds.
- Drimane skeletons offer a promising structural motif for antifungal activity.
Purpose of the Study:
- To optimize mycoleptodiscin A for antifungal properties using core-emulating synthesis.
- To synthesize and evaluate a library of drimane-based heterocycles for antifungal activity.
- To identify novel antifungal leads against key plant pathogenic fungi.
Main Methods:
- Core-emulating optimization strategy for mycoleptodiscin A.
- Synthesis of a diverse library of drimane heterocycles (7 skeletons).
- Antifungal screening against *R. solani*, *P. capsici*, and *S. sclerotiorum*.
Main Results:
- Novel antifungal leads (compounds 3j, 3k, 7a, 7d, 8g) identified against *R. solani*.
- Compound 3e exhibited a distinct antifungal spectrum compared to boscalid against *P. capsici* and *S. sclerotiorum*.
- Drimanyl oxazoline 3e and its hydrolyzate 9a showed significant preventative efficacy against *S. sclerotiorum*.
Conclusions:
- Less complex drimane heterocycles are effective antifungal agents.
- Optimized drimane structures can serve as accessible models for novel antifungal discovery.
- Mechanism of action involves inhibition of oxalic acid production and cell membrane damage.
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