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Molecules 2018, 23(9), 2203; https://doi.org/10.3390/molecules23092203

Investigation of Novel Pesticides with Insecticidal and Antifungal Activities: Design, Synthesis and SAR Studies of Benzoylpyrimidinylurea Derivatives

1
Key Laboratory of Green Prevention and Control of Tropical Plant Diseases and Pests, Hainan University, Haikou 570228, China
2
Institute of Tropical Agriculture and Forestry, Hainan University, Haikou 570228, China
3
School of Chemical & Chemical Engineering, Inner Mongolia University, Hohhot 010021, China
*
Author to whom correspondence should be addressed.
Received: 9 August 2018 / Revised: 25 August 2018 / Accepted: 28 August 2018 / Published: 31 August 2018
(This article belongs to the Section Medicinal Chemistry)
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Abstract

In order to find pesticides with insecticidal and antifungal activities, a series of novel benzoyl pyrimidinylurea derivatives were designed and synthesized. All target compounds were identified by 1H-NMR spectroscopy and HRMS. Insecticidal and antifungal activity of these compounds were evaluated and the structure-activity relationships (SAR) were clearly and comprehensively illustrated. Compound 7, with low toxicity to zebrafish (LC50 = 378.387 µg mL−1) showed 100% inhibition against mosquito (Culex pipiens pallens) at 0.25 µg mL−1. Both compounds 19 and 25 exhibited broad-spectrum fungicidal activity (>50% inhibitory activities against 13 phytopathogenic fungi), which were better than those of the commercial pesticide pyrimethanil (>50% inhibitory activities against eight phytopathogenic fungi). Furthermore, compounds 19 and 25 exhibited protective activity against Sclerotinia sclerotiorum on leaves of Brassica oleracea L. during in vivo experiments. View Full-Text
Keywords: benzoylpyrimidinylurea derivatives; antifungal activity; insecticidal activity; embryo toxicity; zebrafish benzoylpyrimidinylurea derivatives; antifungal activity; insecticidal activity; embryo toxicity; zebrafish
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Chen, P.; Song, X.; Fan, Y.; Kong, W.; Zhang, H.; Sun, R. Investigation of Novel Pesticides with Insecticidal and Antifungal Activities: Design, Synthesis and SAR Studies of Benzoylpyrimidinylurea Derivatives. Molecules 2018, 23, 2203.

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