Design, synthesis, anti-TMV, fungicidal, and insecticidal activity evaluation of 1,2,3,4-tetrahydro-β-carboline-3-carboxylic acid derivatives based on virus inhibitors of plant sources
Design, synthesis, anti-TMV, fungicidal, and insecticidal activity evaluation of 1,2,3,4-tetrahydro-β-carboline-3-carboxylic acid derivatives based on virus inhibitors of plant sources
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DOI：
10.1016/j.bmcl.2014.09.063
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发表时间：
2014-11-15
影响因子：
2.7
通讯作者：
Wang, Qing-min
中科院分区：
文献类型：
--
作者：
Song, Hong-jian;Liu, Yong-xian;Wang, Qing-min
借鉴植物源农药的创制思想，设计合成了一系列四氢-β-咔啉-3-羧酸类化合物，并对其抗烟草花叶病毒、杀菌和杀虫活性进行了初步评价。其中大部分衍生物在体内外均表现出良好的抗烟草花叶病毒活性。尤其是化合物8和15的体内活性高于利巴韦林。化合物8在50 mg/kg的剂量下对花生黑星病、番茄斑点落叶病、玉米小斑病和立枯丝核菌的杀菌率均在70%以上，化合物16和20对粘虫和玉米象的杀菌率均在60%以上。(C)2014爱思唯尔有限公司。保留所有权利。
By drawing the creation ideas of botanical pesticides, a series of tetrahydro-beta-carboline-3-carboxylic acid derivatives were designed and synthesized, and first evaluated for their anti-TMV, fungicidal and insecticidal activities. Most of these derivatives exhibited good antiviral activity against TMV both in vitro and in vivo. Especially, the activities of compounds 8 and 15 in vivo were higher than that of ribavirin. The compound 8 exhibited more than 70% fungicidal activities against Cercospora arachidicola Hori, Alternaria solani, Bipolaris maydis, and Rhizoctonia solani at 50 mg/kg, compounds 16 and 20 exhibited more than 60% insecticidal activities against Mythimna separate and Ostrinia nubilalis. (C) 2014 Elsevier Ltd. All rights reserved.