A novel series of chromenone analogs were synthesized and evaluated for their inhibitory activity against interleukin-5. Among them compounds 5-(cyclohexylmethoxy)-N-(4-hydroxy-3-(hydroxymethyl)phenyl)-4-oxo-4H-chromene-3-carboxamide (8e, 54% inhibiti...
A novel series of chromenone analogs were synthesized and evaluated for their inhibitory activity against interleukin-5. Among them compounds 5-(cyclohexylmethoxy)-N-(4-hydroxy-3-(hydroxymethyl)phenyl)-4-oxo-4H-chromene-3-carboxamide (8e, 54% inhibition at 30 μM) and ethyl 3-(5-(cyclohexylmethoxy)- 4-oxo-4H-chromene-3-carboxamido)benzoate (8g, 62% inhibition at 30 μM) showed the most potent activity. The SAR activity of
these chromenones indicated that the bulky substituents at ring B increases the inhibition against IL-5 though none of the compound showed potent inhibition. The reason for less activity of the chromenones 8a-h may be due to the rigidity of amine linkage.