Tacripyrines, the first tacrine-dihydropyridine hybrids, as multitarget-directed ligands for the treatment of Alzheimer's disease.

@article{MarcoContelles2009TacripyrinesTF,
  title={Tacripyrines, the first tacrine-dihydropyridine hybrids, as multitarget-directed ligands for the treatment of Alzheimer's disease.},
  author={Jos{\'e} Marco-Contelles and Rafael Le{\'o}n and Crist{\'o}bal de Los R{\'i}os and Abdelouahid Samadi and Manuela Bartolini and Vincenza Andrisano and Oscar Huertas and Xavier Barril and F. Javier Luque and Mar{\'i}a Isabel Rodr{\'i}guez-Franco and Beatriz L{\'o}pez and Manuela Garc{\'i}a L{\'o}pez and Antonio G Garc{\'i}a and Maria do Carmo Carreiras and M{\'e}rcedes Villarroya},
  journal={Journal of medicinal chemistry},
  year={2009},
  volume={52 9},
  pages={2724-32}
}
Tacripyrines (1-14) have been designed by combining an AChE inhibitor (tacrine) with a calcium antagonist such as nimodipine and are targeted to develop a multitarget therapeutic strategy to confront AD. Tacripyrines are selective and potent AChE inhibitors in the nanomolar range. The mixed type inhibition of hAChE activity of compound 11 (IC(50) 105 +/- 15 nM) is associated to a 30.7 +/- 8.6% inhibition of the proaggregating action of AChE on the Abeta and a moderate inhibition of Abeta self… CONTINUE READING

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