2. Academic Validation
  3. Promising Fungicides from Allelochemicals: Synthesis of Umbelliferone Derivatives and Their Structure⁻Activity Relationships

Promising Fungicides from Allelochemicals: Synthesis of Umbelliferone Derivatives and Their Structure⁻Activity Relationships

  • Molecules. 2018 Nov 16;23(11):3002. doi: 10.3390/molecules23113002.
Le Pan 1,  Dongyu Lei 2,  Lu Jin 3,  Yuan He 4,  Qingqing Yang 5
Affiliations

Affiliations

  • 1 Chemical Engineering College, Xinjiang Agricultural University, Urumqi 830052, China. [email protected].
  • 2 Department of Physiology, Preclinical School, Xinjiang Medical University, Urumqi 830011, China. [email protected].
  • 3 Chemical Engineering College, Xinjiang Agricultural University, Urumqi 830052, China. [email protected].
  • 4 Chemical Engineering College, Xinjiang Agricultural University, Urumqi 830052, China. [email protected].
  • 5 Chemical Engineering College, Xinjiang Agricultural University, Urumqi 830052, China. [email protected].
PMID: 30453559 DOI: 10.3390/molecules23113002
Abstract

Umbelliferone was discovered to be an important allelochemical in our previous study, but the contribution of its activity and structure has not yet been revealed. In this study, a series of analogues were synthesized to determine the skeleton of umbelliferone and examine its fungicidal activity. Furthermore, targeted modifications were conducted with three plant parasitic fungi to examine the lead compounds. Among those tested, compounds 2f and 10 were found to show excellent Antifungal activity with an inhibitory rate over 80% at 100 ug/mL. The study proves that umbelliferone can be a promising skeleton for fungicides discovery. In addition, the primary structure⁻activity relationship provides a good guidance for the discovery of novel fungicides based on natural products in the future.

Keywords

EC50 values; allelochemical; antifungal activity; umbelliferone derivatives.

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