当前位置： SCI文献检索 > EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY期刊下所有文献 > Base promoted synthesis of novel indole-dithiocarbamate compounds as potential anti-inflammatory therapeutic agents for treatment of acute lung injury.

Base promoted synthesis of novel indole-dithiocarbamate compounds as potential anti-inflammatory therapeutic agents for treatment of acute lung injury.

Abstract：

:An efficient protocol for highly chemoselective introduction of dithiocarbamate groups to nitrogen position of indoles with bis(dialkylaminethiocarbonyl)disulfides was achieved by employing t-BuOK as a promoter. Based on this methodology, twenty nine novel indole-dithiocarbamate compounds were prepared in moderate to excellent yields at room temperature. All compounds were evaluated for their anti-inflammatory activity. Most of the compounds exhibited high potency on inhibiting the releasing of tumor necrosis factor alpha (TNF-α) and interleukin-6 (IL-6). Four of them were found to suppress in vitro cytokine production in a dose-dependent manner with IC50 values in the nanomolar range. Additionally, 3-methyl-1H-indol-1-yl dimethylcarbamodithioate (3o) effectively ameliorated histopathological changes of lung tissues and attenuated lipopolysaccharides (LPS)-induced acute lung injury (ALI) in vivo. These data suggest that the new indole-dithiocarbamate derivatives could be particularly useful for further pharmaceutical development for the treatment of ALI.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Song Z,Zhou Y,Zhang W,Zhan L,Yu Y,Chen Y,Jia W,Liu Z,Qian J,Zhang Y,Li C,Liang G

doi

10.1016/j.ejmech.2019.03.022

subject

Has Abstract

pub_date

2019-06-01 00:00:00

pages

54-65

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(19)30239-9

journal_volume

171

pub_type

杂志文章

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