Synthesis and antifungal activity of novel sulfoxide derivatives containing trimethoxyphenyl substituted 1,3,4-thiadiazole and 1,3,4-oxadiazole moiety

被引：170

作者：

Liu, Fang ^{[1
]}

Luo, Xiao-Qiong ^{[1
]}

Song, Bao-An ^{[1
]}

Bhadury, Pinaki S. ^{[1
]}

Yang, Song ^{[1
]}

Jin, Lin-Hong ^{[1
]}

Xue, Wei ^{[1
]}

Hu, De-Yu ^{[1
]}

机构：

[1] Guizhou Univ, Minist Educ, Ctr Res & Dev Fine Chem, Key Lab Green Pesticide & Bioengn, Guiyang 550025, Peoples R China

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2008年 / 16卷 / 07期

基金：

中国国家自然科学基金;

关键词：

sulfoxides; thioether; antifungal bioactivity; mechanism of action;

D O I：

10.1016/j.bmc.2008.02.006

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：

Selective oxidation of sulfides 7 or 8 to sulfoxides 9 or 10 is achieved by mCPBA. The structures of the compounds 9 or 10 are confirmed by elemental analysis, IR, and H-1 NMR. The bioassay results showed that title compound 10a possess high antifungal activities with EC50 values ranging from 19.91 to 63.97 mu g/mL. The mechanism of action of 10a against Sclerotinia sclerotiorum was studied. After treating with compound 10a at 100 mu g/mL for 12 h, the mycelial reducing sugar, D-GlcNAc, soluble protein and pyruvate content, chitinase activity showed declining tendency. (C) 2008 Elsevier Ltd. All rights reserved.

引用

页码：3632 / 3640

页数：9