Synthesis and biological evaluation of chromone-3-carboxamides

被引：4

作者：

Gordon, Allen T. ^{[1
]}

Ramaite, Isaiah D. I. ^{[1
]}

Mnyakeni-Moleele, Simon S. ^{[1
]}

机构：

[1] Univ Venda, Dept Chem, Private Bag X5050, Thohoyandou, Limpopo, South Africa

来源：

ARKIVOC | 2020年

基金：

新加坡国家研究基金会;

关键词：

Chromones; chromone-3-carboxylic acids; Vilsmeier-Haack formylation; anti-inflammatory; anti-tryponosomal; cytotoxicity; ONE-POT SYNTHESIS; DNA-BINDING; CHROMONE;

D O I：

10.24820/ark.5550190.p011.356

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

The aim of our study was to synthesize novel chromone-3-carboxamides and to conduct biological evaluations in search for lead compounds for the treatment of a range of debilitating disease states. Corresponding 2-hydroxyacetophenones were subjected to Vilsmeier-Haack formylation to give chromone-3-carbaldehydes, which were subsequently oxidised to give chromone-3-carboxylic acids. Treatment of the carboxylic acids with thionyl chloride resulted in the in situ formation of the corresponding acid chlorides, which were reacted with various amines in the presence of triethylamine to give the corresponding novel chromone-3-carboxamides in good yields. Selected chromone derivatives were then evaluated for their anti-inflammatory, anti-tryponosomal and cytotoxic properties. [GRAPHICS] .

引用

页码：148 / 160

页数：13

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