@article{LemkeChristmannYinetal.2019,
  author    = {Carina Lemke and Joscha Christmann and Jiafei Yin and Jos{\´e} M. Alonso and Estefan{\´i}a Serrano and Mourad Chioua and Lhassane Ismaili and Mar{\´i}a Angeles Mart{\´i}nez-Grau and Christopher D. Beadle and Tatiana Vetman and Florian M. Dato and Ulrike Bartz and Paul W. Elsinghorst and Markus Pietsch and Christa E. M{\"u}ller and Isabel Iriepa and Timo Wille and Jos{\´e} Marco-Contelles and Michael G{\"u}tschow},
  title     = {Chromenones as Multineurotargeting Inhibitors of Human Enzymes},
  series   = {ACS Omega},
  volume    = {4},
  number    = {26},
  publisher = {American Chemical Society (ACS)},
  issn      = {2470-1343},
  doi       = {10.1021/acsomega.9b03409},
  url       = {https://nbn-resolving.org/urn:nbn:de:hbz:1044-opus-47081},
  pages     = {22161 -- 22168},
  year      = {2019},
  abstract  = {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 Mitsunobu- or 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 μM, respectively, was achieved with the dual-target 6-(4-(piperidin-1-yl)butoxy)-4H-chromen-4-one (7).},
  language  = {en}
}