Journal
ACS OMEGA
Volume 4, Issue 26, Pages 22161-22168Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acsomega.9b03409
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Funding
- MINECO [SAF2015-65586-R]
- UCJC [2015-12, 2014-35, 2015-21]
- EU (COST Action) [CA15135]
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The complex nature of multifactorial diseases, such as Morbus Alzheimer, has produced a strong need to design multitarget-directed ligands to address the involved complementary pathways. We performed a purposive structural modification of a tetratarget small-molecule, that is contilisant, and generated a combinatorial library of 28 substituted chromen-4-ones. The compounds comprise a basic moiety which is linker-connected to the 6-position of the heterocyclic chromenone core. The syntheses were accomplished by Mitsunobuor Williamson-type ether formations. The resulting library members were evaluated at a panel of seven human enzymes, all of which being involved in the pathophysiology of neurodegeneration. A concomitant inhibition of human acetylcholinesterase and human monoamine oxidase B, with IC50 values of 5.58 and 7.20 mu M, respectively, was achieved with the dual-target 6-(4-(piperidin-1-yl)butoxy)-4H-chromen-4-one (7).
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