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首页> 外文期刊>Letters in drug design & discovery >Synthesis and Fungicidal Activity of N-(2,4,5-trichlorophenyl)-2-Oxo-and 2-Hydroxycycloalkylsulfonamides
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Synthesis and Fungicidal Activity of N-(2,4,5-trichlorophenyl)-2-Oxo-and 2-Hydroxycycloalkylsulfonamides

机译:N-(2,4,5-三氯苯基)-2-氧-和2-羟基环烷基磺酰胺的合成及杀真菌活性

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摘要

A series of N-(2,4,5-trichlorophenyl)-2-Oxo- and 2-Hydroxycycloalkyl- sulfonamides (series II and III) were designed and synthesized based on the leading compound chesulfamide (code name: CAUWL-2004-L-13). Their structures were confirmed by 1H NMR, IR and elemental analysis. Compounds II and III showed excellent activities against the Botrytis cinerea both in vitro and in vivo. Mycelia growth and conidial germination assays exhibited that EC50 of compound IId were 0.64 μg mL-1 and 0.34 μg mL-1 respectively. For in vivo control of B. cinerea in cucumber seedlings, compounds IIb and IId showed better control effect than the commercial fungicides procymidone and pyrimethanil. In addition, these new compounds had broader fungicidal spectra than chlorothalonil. The fungicidal activity was affected obviously by the size of cycloalkane. All the compounds with six-, seven-, and eight-membered ring showed high fungicidal activities.
机译:基于主要化合物chessulfamide(代号:CAUWL-2004-L),设计并合成了一系列N-(2,4,5-三氯苯基)-2-氧-和2-羟基环烷基-磺酰胺(系列II和III) -13)。通过1 H NMR,IR和元素分析证实了它们的结构。化合物II和III在体外和体内均显示出针对灰葡萄孢的优异活性。菌丝体生长和分生孢子萌发试验表明,化合物IId的EC50分别为0.64μgmL-1和0.34μgmL-1。为了体内控制黄瓜幼苗中的灰葡萄孢,化合物IIb和IId显示出比商业杀真菌剂嘧啶酮和嘧啶醇更好的防治效果。另外,这些新化合物具有比百菌清更广的杀菌谱。环烷烃的大小对杀菌活性有明显的影响。具有六元,七元和八元环的所有化合物均显示出较高的杀真菌活性。

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