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含喹唑啉和苯并噻唑基团的新型β-氨基酸酯衍生物的合成及其抗烟草花叶病毒活性

Synthesis and anti-TMV activity of novel β-amino acid ester derivatives containing quinazoline and benzothiazole moieties.

作者信息

Xiao Han, Li Pei, Hu Deyu, Song Bao-An

机构信息

State Key Laboratory Breeding Base of Green Pesticide and Agricultural Bioengineering, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Center for Research and Development of Fine Chemicals, Guizhou University, Guiyang 550025, PR China; School of Chemistry and Environmental Science, Guizhou Minzu University, Guiyang 550025, PR China.

State Key Laboratory Breeding Base of Green Pesticide and Agricultural Bioengineering, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Center for Research and Development of Fine Chemicals, Guizhou University, Guiyang 550025, PR China.

出版信息

Bioorg Med Chem Lett. 2014 Aug 1;24(15):3452-4. doi: 10.1016/j.bmcl.2014.05.073. Epub 2014 Jun 2.

Abstract

Here, a series of β-amino acid ester derivatives containing quinazoline and benzothiazoles was synthesized and evaluated for anti-tobacco mosaic virus (TMV) activity. The compounds 3n, 3o, 3p and 3q showed good antiviral activity against TMV at a concentration of 500 μg/mL, with curative rates of 55.55%, 52.32%, 52.77% and 50.91%, respectively, and protection rates of 52.33%, 55.96%, 54.21% and 50.98%, respectively. These values were close to those of the commercially available antiviral agent ningnanmycin (which has curative and protection rates of 55.27% and 52.16%, respectively). To our knowledge, this is the first report of the anti-TMV activity of β-amino acid ester derivatives containing quinazoline and benzothiazoles moieties; the results indicate that these novel compounds can potentially be used as protective agents against TMV diseases.

摘要

在此,合成了一系列含有喹唑啉和苯并噻唑的β-氨基酸酯衍生物,并对其抗烟草花叶病毒(TMV)活性进行了评估。化合物3n、3o、3p和3q在浓度为500μg/mL时对TMV表现出良好的抗病毒活性,治愈率分别为55.55%、52.32%、52.77%和50.91%,保护率分别为52.33%、55.96%、54.21%和50.98%。这些数值与市售抗病毒剂宁南霉素的数值相近(宁南霉素的治愈率和保护率分别为55.27%和52.16%)。据我们所知,这是首次报道含有喹唑啉和苯并噻唑部分的β-氨基酸酯衍生物的抗TMV活性;结果表明,这些新型化合物有可能用作预防TMV病害的保护剂。

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