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Séminaire Chimie IBMM/ED459

Tacripyrines, as new multi-target-directed ligands for the potential treatment of Alzheimer’s disease

Prof. José Luis Marco-Contelles (Laboratorio de Quimica Médica, Instituto de Química Orgánica General – CSIC, Madrid, Spain)

publié le , mis à jour le

Le Mercredi 10 Juillet 2013 à 09h45
UM2, salle de cours SC-16.01

Tacripyrines (tacrine-dihydropyridine hybrids) 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 Alzheimer’s Disease (AD). Tacripyrines are selective and potent AChE inhibitors in the nanomolar range. The mixed type inhibition of hAChE activity of « p-methoxytacripyrine » (IC50 105±15 nM) is associated to a 30.7±8.6% inhibition of the proaggregating action of AChE on the Aβ, and a moderate inhibition of Aβ self-aggregation (34.9±5.4%). Tacripyrines are neuroprotective agents, show moderate Ca2+ channel blocking effect, and cross the blood-brain barrier, emerging as lead candidates for treating AD.

Contact local IBMM : Dr. Evelina Colacino, Dr. Frédéric Lamaty (DAPP)

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