Person: Sollhuber Kretzer, Mónica
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First Name
Mónica
Last Name
Sollhuber Kretzer
Affiliation
Universidad Complutense de Madrid
Faculty / Institute
Farmacia
Department
Química en Ciencias Farmacéuticas
Area
Química Orgánica
Identifiers
1 results
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Item Analogues of cannabinoids as multitarget drugs in the treatment of Alzheimer’s disease(European Journal of Pharmacology, 2021) Fernandez, María; Villaro, Wilma; Gómez Cañas, María; García-Arencibia, Moisés; Egea, Javier; Fernández Ruiz, José Javier; Martín, María Isabel; Girón, Rocío; Sánchez Montero, José; Agis Torres, Ángel; Solano, David; Sollhuber Kretzer, Mónica; Sánchez Montero, JoséGiven that neuronal degeneration in Alzheimer's disease (AD) is caused by the combination of multiple neurotoxic insults, current directions in the research of novel therapies to treat this disease attempts to design multitarget strategies that could be more effective than the simply use of acetylcholinesterase inhibitors; currently, the most used therapy for AD. One option, explored recently, is the synthesis of new analogues of cannabinoids that could competitively inhibit the acetylcholinesterase (AChE) enzyme and showing the classic neuroprotective profile of cannabinoid compounds. In this work, molecular docking has been used to design some cannabinoid analogues with such multitarget properties, based on the similarities of donepezil and Δ9-tetrahydrocannabinol. The analogues synthesized, compounds 1 and 2, demonstrated to have two interesting characteristics in different in vitro assays: competitive inhibition of AChE and competitive antagonism at the CB1/CB2 receptors. They are highly lipophilic, highlighting that they could easily reach the CNS, and apparently presented a low toxicity. These results open the door to the synthesis of new compounds for a more effective treatment of AD.