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Open AccessArticle

Design, Synthesis and Antifungal Activity of Novel Benzoylcarbamates Bearing a Pyridine Moiety

1
College of Chemistry and Material Science, Shandong Agricultural University, Tai’an 271018, China
2
College of Agronomy, Shandong Agricultural University, Tai’an 271018, China
*
Author to whom correspondence should be addressed.
Appl. Sci. 2018, 8(12), 2577; https://doi.org/10.3390/app8122577
Received: 1 November 2018 / Revised: 5 December 2018 / Accepted: 8 December 2018 / Published: 11 December 2018
(This article belongs to the Section Chemistry)
Many natural and synthetic pyridine derivatives have good biological activity, and are widely used in the fields of pesticides and medicines. On the other hand, carbamate fungicides possess some unique properties, such as high efficiency, strong selectivity, low toxicity, and environmental friendliness, and are often used to control many plant diseases. Therefore, discovering novel pyridine-based carbamates is of great significance. In this paper, we chose the excellent fungicides tolprocarb and picarbutrazox as lead compounds, integrating benzoyl, carbamate, and pyridinyl moieties into a molecule. Thus, we designed and synthesized a series of substituted benzoyl carbamates containing a pyridine ring, and evaluated the in vitro antifungal activity. The target compounds exhibited moderate to strong bioactivity against Botrytis cinerea, among which the compounds 4d, 4f, 4g, and 4h exhibited significant activity with EC50 values (the concentration resulting in a 50% inhibition) of 6.45–6.98 μg/mL, and their activities were near or superior to that of chlorothalonil. Additionally, 4h exhibited moderate activity against Sclerotinia sclerotiorum with an EC50 value of 10.85 μg/mL. View Full-Text
Keywords: pyridine; benzoyl; carbamate; synthesis; bioactivity; antifungal activity pyridine; benzoyl; carbamate; synthesis; bioactivity; antifungal activity
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MDPI and ACS Style

Wan, F.-X.; Wang, J.-H.; Shi, Y.-H.; Niu, L.-Z.; Jiang, L. Design, Synthesis and Antifungal Activity of Novel Benzoylcarbamates Bearing a Pyridine Moiety. Appl. Sci. 2018, 8, 2577.

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