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Benzophenone Derivatives with Histamine H₃ Receptor Affinity and Cholinesterase Inhibitory Potency as Multitarget-Directed Ligands for Possible Therapy of Alzheimer's Disease.

ABSTRACT: The multitarget-directed ligands demonstrating affinity to histamine H₃ receptor and additional cholinesterase inhibitory potency represent a promising strategy for research into the effective treatment of Alzheimer's disease. In this study, a novel series of benzophenone derivatives was designed and synthesized. Among these derivatives, we identified compound 6 with a high affinity for H₃R (K_i = 8 nM) and significant inhibitory activity toward BuChE (IC₅₀ = 172 nM and 1.16 µM for eqBuChE and hBuChE, respectively). Further in vitro studies revealed that compound 6 (4-fluorophenyl) (4-((5-(piperidin-1-yl)pentyl)oxy)phenyl)methanone) displays moderate metabolic stability in mouse liver microsomes, good permeabilit

SUBMITTER: Godyn J

PROVIDER: S-EPMC9822066 | biostudies-literature | 2022 Dec

REPOSITORIES: biostudies-literature

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Benzophenone Derivatives with Histamine H₃ Receptor Affinity and Cholinesterase Inhibitory Potency as Multitarget-Directed Ligands for Possible Therapy of Alzheimer's Disease.

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Benzophenone Derivatives with Histamine H3 Receptor Affinity and Cholinesterase Inhibitory Potency as Multitarget-Directed Ligands for Possible Therapy of Alzheimer's Disease.

OmicsDI is part of the ELIXIR infrastructure

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Benzophenone Derivatives with Histamine H₃ Receptor Affinity and Cholinesterase Inhibitory Potency as Multitarget-Directed Ligands for Possible Therapy of Alzheimer's Disease.