Small Changes Result in Large Differences: Discovery of (鈭?-Incrustoporin Derivatives as Novel Antiviral and Antifungal Agents

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• 作者：Aidang Lu ; Jinjin Wang ; Tengjiao Liu ; Jian Han ; Yinhui Li ; Min Su ; Jianxin Chen ; Hui Zhang ; Lizhong Wang ; Qingmin Wang
• 刊名：Journal of Agricultural and Food Chemistry
• 出版年：2014
• 出版时间：September 3, 2014
• 年：2014
• 卷：62
• 期：35
• 页码：8799-8807
• 全文大小：262K
• ISSN：1520-5118

文摘

On the basis of the structure of natural product (鈭?-incrustoporin (1), a series of lactone compounds 4a鈥?b>i and 5a鈥?b>i were designed and synthesized from nitroolefin. The antiviral and antifungal activities of these compounds were evaluated in vitro and in vivo. The small changes between 4 and 5 at the 3,4-position result in large differences in bioactivities. Compounds 4 exhibited significantly higher antiviral activity against tobacco mosaic virus (TMV) than dehydro compounds 5. However, the antifungal activity of 4 is relatively lower than that of 5. Compounds 4a, 4c, and 4i with excellent in vivo anti-TMV activity emerged as new antiviral lead compounds. Compounds 5d鈥?b>g showed superiority over the commercial fungicides chlorothalonil and carbendazim against Cercospora arachidicola Hor at 50 mg kg^鈥?. The present study provides fundamental support for the development and optimization of (鈭?-incrustoporin derivatives as potential inhibitors of plant virus and pathogenic fungi.

Keywords:

2,5-dihydrofuran-2-ones; (鈭?-incrustoporin derivatives; anti-TMV; antifungal activity