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ID: ALA4376837
Journal: J Med Chem
Title: New Dual Small Molecules for Alzheimer's Disease Therapy Combining Histamine H3 Receptor (H3R) Antagonism and Calcium Channels Blockade with Additional Cholinesterase Inhibition.
Authors: Malek R, Arribas RL, Palomino-Antolin A, Totoson P, Demougeot C, Kobrlova T, Soukup O, Iriepa I, Moraleda I, Diez-Iriepa D, Godyń J, Panek D, Malawska B, Głuch-Lutwin M, Mordyl B, Siwek A, Chabchoub F, Marco-Contelles J, Kiec-Kononowicz K, Egea J, de Los Ríos C, Ismaili L.
Abstract: New tritarget small molecules combining Ca2+ channels blockade, cholinesterase, and H3 receptor inhibition were obtained by multicomponent synthesis. Compound 3p has been identified as a very promising lead, showing good Ca2+ channels blockade activity (IC50 = 21 ± 1 μM), potent affinity against hH3R (Ki = 565 ± 62 nM), a moderate but selective hBuChE inhibition (IC50 = 7.83 ± 0.10 μM), strong antioxidant power (3.6 TE), and ability to restore cognitive impairment induced by lipopolysaccharide.
CiteXplore: 31724859