Natural products as sources of new fungicides (III): Antifungal activity of 2,4-dihydroxy-5-methylacetophenone derivatives

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• 作者：Wei Shi ; Wen-Jia Dan ; Jiang-Jiang Tang ; Yan Zhang ; Tseden Nandinsuren ; An-Ling Zhang ; Jin-Ming Gao ; ^{jinminggao@nwsuaf.edu.cn" class="auth_mail" title="E-mail the corresponding author}
• 关键词：Natural products ; Agrochemicals ; Acetophenone derivatives ; Phytopathogenic fungi ; Antifungal agents ; Structure&ndash ; activity relationship
• 刊名：Bioorganic & Medicinal Chemistry Letters
• 出版年：2016
• 出版时间：1 May 2016
• 年：2016
• 卷：26
• 期：9
• 页码：2156-2158
• 全文大小：385 K

文摘

A series of new 2,4-dihydroxy-5-methylacetophenone rong class="boldFont">2rong> derivatives were synthesized, and characterized by ¹H, ¹³C NMR and ESI-MS. Their antifungal activities were evaluated in vitro against five important plant fungal pathogens including Cytospora sp., Glomerella cingulate, Pyricularia oryzaecar, Botrytis cinerea and Alternaria solani by the mycelial growth inhibitory rate assay. Compounds rong class="boldFont">2brong>–rong class="boldFont">drong>, rong class="boldFont">2grong> and rong class="boldFont">2hrong> displayed a broad-spectrum activity. The log P value of these active compounds is ranging from 1.71 to 2.54. Especially, isopropyl ketone rong class="boldFont">2grong> (log P 2.27) was found to be the most active to the tested organisms with IC₅₀ values of 17.28–32.32 μg/mL. The results suggest that compound rong class="boldFont">2grong> might be a promising candidate in the development of new agrochemical antifungal agents. Preliminary structure–activity relationship (SAR) studies of the acetophenone derivatives are also discussed.