Studies on the affinity of 6-[(: N -(cyclo)aminoalkyl)oxy]-4 H -chromen-4-ones for sigma 1/2 receptors

Sigma represent attractive targets for the development of potential agents for the treatment of neurodegenerative disorders. In search of multitarget small molecules (MSMs) against Morbus Alzheimer and related diseases, we have discovered that 6-(4-(piperidin-1-yl)butoxy)-4H-chromen-4-one (7), a previously identified MSM with potent dual-target activities against acetylcholinesterase and monoamine oxidase B, exhibited S1/S2 receptor modulatory activity. A further chromenone, 6-((5-morpholinopentyl)oxy)-4H-chromen-4-one (12), was identified to be almost equipotent to S1RA, an established 1 receptor antagonist.