Novel tacrine-grafted Ugi adducts as multipotent anti-Alzheimer drugs: a synthetic renewal in tacrine-ferulic acid hybrids.

@article{Benchekroun2015NovelTU,
  title={Novel tacrine-grafted Ugi adducts as multipotent anti-Alzheimer drugs: a synthetic renewal in tacrine-ferulic acid hybrids.},
  author={Mohamed Benchekroun and Manuela Bartolini and Javier Egea and Alejandro Romero and Elena Soriano and Marc Pudlo and Vincent Luzet and Vincenza Andrisano and Mar{\'i}a-Luisa Jimeno and Manuela Garc{\'i}a L{\'o}pez and Sarah Wehle and Tijani Gharbi and Bernard Refouvelet and Luc{\'i}a de Andr{\'e}s and Clara Herrera-Arozamena and Barbara Monti and Maria Laura Bolognesi and Mar{\'i}a Isabel Rodr{\'i}guez-Franco and Michael Decker and Jos{\'e} Marco-Contelles and Lhassane Ismaili},
  journal={ChemMedChem},
  year={2015},
  volume={10 3},
  pages={523-39}
}
Herein we describe the design, multicomponent synthesis, and biological, molecular modeling and ADMET studies, as well as in vitro PAMPA-blood-brain barrier (BBB) analysis of new tacrine-ferulic acid hybrids (TFAHs). We identified (E)-3-(hydroxy-3-methoxyphenyl)-N-{8[(7-methoxy-1,2,3,4-tetrahydroacridin-9-yl)amino]octyl}-N-[2-(naphthalen-2-ylamino)2-oxoethyl]acrylamide (TFAH 10 n) as a particularly interesting multipotent compound that shows moderate and completely selective inhibition of human… CONTINUE READING
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The Organic Chemistry of Enzyme- Catalyzed Reactions

R. B. Silverman
Academic Press, San Diego • 2000
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