Synthesis, Antiviral and Antifungal Bioactivity of2-Cyano-acrylate Derivatives Containing Phosphonyl Moieties

Molecules

Yin-Pu Lv²  Xian-You Wan²  Bao-An Song¹  Song Yang²  Kai Yan²  Guang-Fang Xu²  Pinaki S Bhadury²  Fang Liu²  Lin-Hong Jin² 

[1] id="af1-molecules-12-00965">Center for Research and Development of Fine Chemicals, Guizhou University, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Guiyang, 550025, P. R. Chi

关键词: 2-Cyanoacrylate;    phosphonyl moiety;    antiviral activity;    antifungal activity;    synthesis;   

DOI  :  10.3390/12050965

来源: mdpi

【 摘 要 】

Alkyl 2-cyano-3-methylthio-3-phosphonylacrylates were synthesized by the reaction of alkyl 2-cyano-3,3-dimethylthioacrylates with dialkyl phosphites. The structures of the new compounds were characterized by elemental analyses, IR, ¹H-, ¹³C- and ³¹P-NMR spectral data. These compounds were tested in vitro against pathogenic fungi, namely, Fusarium graminearum, Cytospora mandshurica and Fusarium oxysporum. Amongst all compounds, 2d and 2t were found to be effective against the tested fungi at 50 µg/mL. A half-leaf method was used to determine the in vivo protective, inactivation and curative efficacies of the title products against tobacco mosaic virus (TMV). Title compounds 2a and 2b were found to possess good in vivo curative, protection and inactivation effects against TMV with inhibitory rates at 500 mg/L of 60.0, 89.4 and 56.5 and 64.2, 84.2 and 61.2 %, respectively. To the best of our knowledge, this is the first report on the antiviral and antifungal activity of alkyl 2-cyano-3-methylthio-3- phosphonylacrylates.

【 授权许可】

Unknown   
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