New Pyrimidine and Pyridine Derivatives as Multitarget Cholinesterase Inhibitors: Design, Synthesis, and <i>In Vitro</i> and <i>In Cellulo</i> Evaluation
Martina Bortolami, Fabiana Pandolfi, Valeria Tudino, Antonella Messore, Valentina Noemi Madia, Daniela De Vita, Roberto Di Santo, Roberta Costi, Isabella Romeo, Stefano Alcaro, Marisa Colone, Annarita Stringaro, Alba Espargaró, Raimon Sabaté, Luigi Scipione
Abstract
and tau, respectively). Moreover, the most active compounds showed low cytotoxicity on a human brain cell line and they were predicted as BBB-permeable.
Topics & Concepts
ButyrylcholinesteraseChemistryPyrimidineAcetylcholinesteraseElectrophorusStereochemistryActive siteCholinesterasePyridineDocking (animal)EnzymeAchéBiochemistryPharmacologyMedicinal chemistryAcetylcholine receptorBiologyNursingTorpedoReceptorMedicineCholinesterase and Neurodegenerative DiseasesComputational Drug Discovery MethodsPesticide Exposure and Toxicity