Abstract
A series of novel thiochroman-4-one derivatives incorporating carboxamide and 1, 3, 4-thiadiazole thioether moieties were synthesized. Bioassay results indicated that the EC50 values of compound 6-chloro-N-(5-(methylthio)-1, 3, 4-thiadiazol-2-yl)-4-oxothiochromane-2-carboxamide (5a) against Xanthomonas oryzae pv. Oryzae (Xoo) and Xanthomonas axonopodis pv. Citri (Xac) were 24 and 30 μg/mL, respectively, which were even better than those of bismerthiazol and thiadiazole copper. Meanwhile, compound 6-methyl-4-oxo-N-(5-(propylthio)-1, 3, 4-thiadiazol-2-yl)thiochromane-2-carboxamide (5m) showed a better antifungal activity against Botrytis cinerea (B. cinerea), with an inhibition rate of 69%, than carbendazim. As far as we know, this is the first report on the antibacterial and antifungal activities of this series of novel thiochroman-4-one derivatives incorporating carboxamide and 1, 3, 4-thiadiazole thioether moieties.
Highlights
Global food safety/security will remain a worldwide concern for the 50 years and beyond
Pesticide application has been a conventional methodology used in plant protection, frequent use of conventional chemical pesticides has resulted in problems in resistance to bacteria and fungi populations, environmental contamination, and human health [2]
With the improvement of human living standards and human health, the demand for high-quality agricultural products as foods makes it necessary to limit the use of conventional chemical pesticides and challenges the control of plant bacterial and fungal diseases [3]. erefore, the current paradigm of relying almost exclusively on conventional chemical pesticides for bacterial and fungal diseases of plants control may need to be reconsidered
Summary
Global food safety/security will remain a worldwide concern for the 50 years and beyond. Bacterial and fungal diseases of plants have been an enormous impact on the food safety/security at various stages of the food chain from primary production to consumption and have presented serious threats in agricultural production and caused enormous economic losses each year worldwide [1]. With the improvement of human living standards and human health, the demand for high-quality agricultural products as foods makes it necessary to limit the use of conventional chemical pesticides and challenges the control of plant bacterial and fungal diseases [3]. Erefore, the current paradigm of relying almost exclusively on conventional chemical pesticides for bacterial and fungal diseases of plants control may need to be reconsidered. Erefore, natural products can either be used directly in bacterial and fungal control or develop novel synthetic analogs with favorable biological properties. We disclosed a series of novel thiochroman-4-one derivatives (Figure 1) which showed moderate to good antibacterial and antifungal activities [11,12,13,14]
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