Tổng hợp các dimethylmaleimide chứa N-substituted và hoạt tính chống nấm của chúng đối với Sclerotinia sclerotiorum

Springer Science and Business Media LLC - Tập 86 - Trang 353-360 - 2012
Zhenzhong Shen1, Yongxian Fan1, Fuge Li1, Xiaolong Chen1, Yinchu Shen1
1Institute of Fermentation Engineering, College of Biological and Environmental Engineering, Zhejiang University of Technology, Hangzhou, People’s Republic of China

Tóm tắt

Các hợp chất chứa maleimide, cả tự nhiên và tổng hợp, có hoạt tính sinh học tốt, đặc biệt là hoạt tính chống nấm. Để điều tra hoạt tính chống nấm của các dimethylmaleimide, 17 dimethylmaleimide chứa N-substituted đã được chuẩn bị từ phản ứng của 2,3-dimethylmaleic anhydride và amin bằng phương pháp tổng hợp đơn giản trong bài báo này. Các hợp chất này đã được đánh giá về hoạt tính chống nấm đối với Sclerotinia sclerotiorum bằng phương pháp đo tốc độ sinh trưởng mycelium. Chúng thể hiện nồng độ ức chế tối thiểu (MIC) dao động từ 0.01–50.0 μg/mL, trong đó N-(2-benzimidazole)-3,4-dimethylmaleimide là hoạt chất mạnh nhất với MIC là 0.01 μg/mL. Mối quan hệ giữa cấu trúc và hoạt tính của những hợp chất này chỉ ra rằng tính kỵ nước của các nhóm N-substituents có liên quan đến hoạt tính chống nấm của chúng. So với các thuốc chống nấm hiện tại, hầu hết các dimethylmaleimide chứa N-substituted có hoạt tính tuyệt vời để kiểm soát S. sclerotiorum và độc tính thấp.

Từ khóa

#dimethylmaleimide #N-substituted #hoạt tính chống nấm #Sclerotinia sclerotiorum #nồng độ ức chế tối thiểu (MIC)

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