Synthesis, structure, and biological activity of novel (oxdi/tri)azoles derivatives containing 1,2,3-thiadiazole or methyl moiety

被引：97

作者：

Liu, Xing-Hai ^{[1
]}

Pan, Li ^{[2
]}

Weng, Jian-Quan ^{[1
]}

Tan, Cheng-Xia ^{[1
]}

Li, Yong-Hong ^{[2
]}

Wang, Bao-Lei ^{[2
]}

Li, Zheng-Ming ^{[2
]}

机构：

[1] Zhejiang Univ Technol, Coll Chem Engn & Mat Sci, Hangzhou 310014, Zhejiang, Peoples R China

[2] Nankai Univ, State Key Lab Elementoorgan Chem, Tianjin 300071, Peoples R China

来源：

MOLECULAR DIVERSITY | 2012年 / 16卷 / 02期

关键词：

1,2,4-Triazole; 1,3,4-Oxidiazole; Crystal structure; Herbicidal activity; KARI activity; KETOL-ACID REDUCTOISOMERASE; ACETOHYDROXYACID SYNTHASE; ISOMEROREDUCTASE; INHIBITORS; BIOACTIVITY; BINDING; SITE;

D O I：

10.1007/s11030-011-9352-z

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

To develop novel inhibitors of ketol-acid reductoisomerase, a series of (oxdi/tri)azoles derivatives was synthesized and characterized by H-1 NMR, MS, elemental analyses, and crystallography. According to the biological activities of these compounds obtained both in vivo and in vitro, compound 4-cyclopropyl-3-((4-fluorobenzyl)thio)-5-methyl-4H-1,2,4-triazole showed excellent KARI inhibitory activity (100% at 100 mu g mL (-1) in vitro). In addition, most of the title compounds exhibited good herbicidal activity against Brassica campestris in vivo.

引用

页码：251 / 260

页数：10

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