4.6 Article

Design, Synthesis, and Bioactivity Evaluation of New Thiochromanone Derivatives Containing a Carboxamide Moiety

Journal

MOLECULES
Volume 26, Issue 15, Pages -

Publisher

MDPI
DOI: 10.3390/molecules26154391

Keywords

thiochromanone; carboxamide; antibacterial activity; antifungal activity

Funding

  1. National Key R&D Program of China [2017YFD0200903]
  2. Science and Technology Foundation of Guizhou Province [ZK [2021]137, [2020]1Y130]
  3. Kaili University Doctoral Program [BS201811]
  4. Science and Technology Platform and Talent Team Project of Guizhou Province [[2018]5251]
  5. Talent Base of Fermentation Engineering and Liquor Making in Guizhou Province [[2018]3]
  6. Zunyi City Innovative Talent Team Program Project [[2020]9]
  7. Excellent Young Scientific and Technological Talent Program [[2019]5645]

Ask authors/readers for more resources

In this study, a series of novel thiochromanone derivatives containing a carboxamide moiety were synthesized and evaluated for their in vitro antibacterial and antifungal activities. Some of the compounds exhibited moderate to good activities against Xanthomonas oryzae pv. oryzae, Xanthomonas oryzae pv. oryzicolaby, Xanthomonas axonopodis pv. citri, Botryosphaeria dothidea, Phomopsis sp., and Botrytis cinerea. Compound 4e showed excellent antibacterial activity against the Xoo, Xoc, and Xac strains, while compound 3b demonstrated moderate antifungal activity against B. dothidea.
In this study, using the botanical active component thiochromanone as the lead compound, a total of 32 new thiochromanone derivatives containing a carboxamide moiety were designed and synthesized and their in vitro antibacterial activities against Xanthomonas oryzae pv. oryzae (Xoo), Xanthomonas oryzae pv. oryzicolaby (Xoc), and Xanthomonas axonopodis pv. citri (Xac) were determined, as well as their in vitro antifungal activities against Botryosphaeria dothidea (B. dothidea), Phomopsis sp., and Botrytis cinerea (B. cinerea). Bioassay results demonstrated that some of the target compounds exhibited moderate to good in vitro antibacterial and antifungal activities. In particular, compound 4e revealed excellent in vitro antibacterial activity against Xoo, Xoc, and Xac, and its EC50 values of 15, 19, and 23 mu g/mL, respectively, were superior to those of Bismerthiazol and Thiodiazole copper. Meanwhile, compound 3b revealed moderate in vitro antifungal activity against B. dothidea at 50 mu g/mL, and the inhibition rate reached 88%, which was even better than that of Pyrimethanil, however, lower than that of Carbendazim. To the best of our knowledge, this is the first report on the antibacterial and antifungal activities of this series of novel thiochromanone derivatives containing a carboxamide moiety.

Authors

I am an author on this paper
Click your name to claim this paper and add it to your profile.

Reviews

Primary Rating

4.6
Not enough ratings

Secondary Ratings

Novelty
-
Significance
-
Scientific rigor
-
Rate this paper

Recommended

No Data Available
No Data Available