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Studies on antianaphylactic agents. 4. Synthesis and structure-activity relationships of 3-(4-oxo-4H-1-benzopyran-3)acrylic acids, a new series of antiallergic substances, and some related compounds

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TLDR
The syntheses of trans-3-(4-oxo-4H-1-benzypyran-3)acrylic acid and a number of analogs shown to be highly active in antiallergic bioassays are described and are of possible value in the treatment of asthma.
Abstract
The syntheses of trans-3-(4-oxo-4H-1-benzypyran-3)acrylic acid and a number of analogs shown to be highly active in antiallergic bioassays are described. These compounds are of possible value in the treatment of asthma. The structural requirements for biological activity are discussed with reference to the type of the substituents on the chromone ring or positions of linkage of the acrylic acid on the pyrone ring.

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Journal ArticleDOI

Chromone: A Valid Scaffold in Medicinal Chemistry

TL;DR: This work was supported by the Foundation for Science and Technology (FCT), Portugal (projects PTDC/QUI-QUI/113687/2009 and PEst-C/QUI/UI0081/2013) and SFRH/BD/61262/2009.
Journal ArticleDOI

Palladium(II)-Catalyzed Direct Intermolecular Alkenylation of Chromones

Donghee Kim, +1 more
- 28 Jul 2011 - 
TL;DR: A new efficient method for the direct alkenylation of chromones via a palladium(II)-catalyzed C-H functionalization reaction was developed and afforded various 3-vinylchromone derivatives, which are privileged structures in many biologically active compounds and versatile synthetic building blocks.
Journal ArticleDOI

Asymmetric Diels–Alder reaction of β,β-disubstituted enals and chromone-fused dienes: construction of collections with high molecular complexity and skeletal diversity

TL;DR: An asymmetric inverse-electron-demand Diels–Alder reaction of chromone-fused dienes and β,β-disubstituted α, β-unsaturated aldehydes has been developed via dienamine catalysis, allowing for the efficient construction of caged or fused tetrahydroxanthones with high molecular complexity and skeletal diversity in excellent diastereo- and enantioselectivities.
Journal ArticleDOI

Chemistry of 4-Oxo-4H-[1]benzopyran-3-carboxaldehyde

TL;DR: The authors present an examen approfondi de la synthese, des proprietes et des reactions de l'oxo-4 chromenecarbaldehyde-3 and l'utilisation de ses condensats for the preparation of divers systemes chimiques.
Journal ArticleDOI

A chromone analog inhibits TNF-alpha induced expression of cell adhesion molecules on human endothelial cells via blocking NF-kappaB activation.

TL;DR: To elucidate the molecular mechanism of inhibition of cell adhesion molecules, the status of nuclear transcription factor-kappaB was investigated and it was established that compound 8a significantly blocked the TNF-alpha induced activation of NF-k KappaB.
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