Design and synthesis of novel hydroxyalkylaminomethylchromones for their IL-5 inhibitory activity

Bioorganic & Medicinal Chemistry
Pillaiyar ThanigaimalaiSang-Hun Jung

Abstract

A series of hydroxyalkylaminomethylchromone analogs 3 were prepared and evaluated as inhibitors of interleukin-5. The most active analog 3d inhibited interleukin-5 activity with an IC₅₀ of 17.5 μM. The structural requirements of chromone analogs possessing the inhibitory activity against IL-5 could be summarized as: (i) the cyclohexylmethoxy group at 5th position of the A ring, (ii) the planarity of chromone ring, (iii) hydrophobic unit around the B ring with hydroxyl functional group, (iv) the hydrophobic unit which does not have to be a planar and (v) the length of carbon units between amino and hydroxyl group is limited to two.

References

Oct 17, 2003·Current Drug Targets. Inflammation and Allergy·Joerg Mattes, Paul S Foster

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Citations

Oct 9, 2013·SAR and QSAR in Environmental Research·M Konstantinidou, D Hadjipavlou-Litina
Jul 4, 2012·International Journal of Molecular Sciences·Santosh Kumar, Joonseok Koh
Oct 31, 2012·Archiv der Pharmazie·Agata Szulawska-MroczekAndrzej Stanczak
Oct 21, 2016·ChemMedChem·Carlos F M SilvaArtur M S Silva
Feb 22, 2014·Chemical Reviews·Alexandra GasparFernanda Borges

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