A series of (Z)-2-benzylidenebenzofuran-3-(2H)-ones (aurones) bearing a variety of substituents on rings A and B were synthesized and evaluated for their antiparasitic activity against the intracellular amastigote form of Leishmania infantum and their cytotoxicity against human THP1-differentiated macrophages. In general, aurones bearing no substituents on ring A (compounds 4a-4f) exhibit highe...

The oxidative cyclisation reactions of 2’-hydroxychalcones to corresponding aurones and flavones are discussed. While Hg2+, Cu2+ and Tl3+-mediated oxidative cyclisation of 2’-hydroxychalcones selectively give aurones, I2, Se4+, In3+, Cu+ and Fe3+-mediated reactions preferable give flavones. The general mechanisms of these oxidative cyclisation reactions are proposed.

A series of 2'-hydroxy-chalcones and their oxidative cyclization products, aurones, have been synthesized and tested for their antioxidant and lipoxygenase inhibitory activity. The natural product aureusidin (31) was synthesized in high yield by a new approach. An extensive structure-relationship study was performed and revealed that several chalcones and aurones possess an appealing pharmacolo...

We have identified naturally occurring 2-benzylidenebenzofuran-3-ones (aurones) as new templates for non-nucleoside hepatitis C virus (HCV) RNA-dependent RNA polymerase (RdRp) inhibitors. The aurone target site, identified by site-directed mutagenesis, is located in thumb pocket I of HCV RdRp. The RdRp inhibitory activity of 42 aurones was rationally explored in an enzyme assay. Molecular docki...

A series of aurones was analyzed for the ability to inhibit respiratory functions of mitochondria of Leishmania parasites. The aim of this study was to find a rational explanation for the activity of certain aurones and auronols as novel antiprotozoal compounds of plant origin. In a cell-free assay mitochondrial fumarate reductase from L. donovani was inhibited in a concentration-dependent mann...

BACKGROUND Aurones are naturally occurring compounds that belong to flavenoids family and have antiplasmodial effects. This study investigated some new aurones derivatives against chloroquine sensitive Plasmodium falciparum. Here we report the synthesis, in vitro antiplasmodial activity and cytotoxic evaluation of 11 compound from derivatives of (Z)-2- benzylidene-4, 6-dimethoxybenzofuran-3(2H)...

The reaction of phenols with 7a led to the synthesis of aurones, while the reaction of phenols with 7b led to the synthesis of flavones.

Flower colour is mainly due to the presence and type of pigments. Pollinator preferences impose selection on flower that ultimately acts Knowing how pollinators perceive flowers with different pigments becomes crucial for a comprehensive understanding plant-pollinator communication evolution. Based space models, we studied whether main groups pollinators, specifically hymenopterans, dipterans, ...

The ability to synthesize arrays of related compounds quickly and with good purity has become critical for a rapid exploration their properties biological or material applications. While number methods have been developed enable this combinatorial synthesis, the existing options were not readily appliable synthesis aurones using simple Knoevenagel condensation approach. In order avoid time, exp...

Aurones are minor flavonoids that possess a wide variety of bioactivity, including antioxidant, anticancer, and enzyme inhibitory activity. L-proline-based natural deep eutectic solvents (NaDES) were synthesized applied as catalysts for the Knoevenagel condensation reaction between benzofuranone substituted benzaldehydes to produce aurones in high yields purity. The vanillin served model reacti...