Design, Synthesis and Bioactivity of Novel 2-Aryl-4-alkylthiazole-5-carboxylic Acid Derivatives

被引：4

作者：

Zhu, Youquan ^{[1
]}

Wang, Danyang ^{[1
]}

Yuan, Yanwei ^{[1
]}

Ma, Yuan ^{[1
]}

Zou, Xiaomao ^{[1
]}

Yang, Huazheng ^{[1
]}

机构：

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

来源：

CHINESE JOURNAL OF ORGANIC CHEMISTRY | 2012年 / 32卷 / 11期

基金：

中国国家自然科学基金;

关键词：

1,3-thiazole; active sub-structure; phenoxyacetate; thifluzamide; fungicidal activity; herbicidal activity; HERBICIDAL ANALOGS;

D O I：

10.6023/cjoc201207004

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

To find new lead compounds with muti-bioactivities, a series of novel 1,3-thiazole-5-carboxylic acid derivatives containing aryloxyacetate were designed via the method of linking active sub-structures, in which the aryloxyacetate with multi-bioactivity was combined to the 1,3-thiazole moiety of ethaboxam, metsulfovax and thifluzamide. The target compounds were synthesized from beta-keto acid ester and 4-hydroxybenzothioamide in 6 steps. Their structures were confirmed by H-1 NMR, IR and HRMS techniques. The preliminary bioassay results indicated that some compounds showed obvious inhibition effects against Fusarium graminearum, and the fungicidal activity of 1j is 52% at 50 mu g/mL.

引用

页码：2115 / 2121

页数：7