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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 <b>6</b> with a high affinity for H₃R (<i>K_i</i> = 8 nM) and significant inhibitory activity toward BuChE (IC₅₀ = 172 nM and 1.16 µM for <i>eq</i>BuChE and <i>h</i>BuChE, respectively). Further in vitro studies revealed that compound <b>6</b> (4-fluorophenyl) (4-((5-(piperidin-1-yl)pentyl)oxy)phenyl)methanone) displays moderate metabolic stability in mouse liver microsomes, good permeability with a permeability coefficient value (P_e) of 6.3 × 10⁻⁶ cm/s, and its safety was confirmed in terms of hepatotoxicity in the HepG2 cell line. Therefore, we investigated the in vivo activity of compound <b>6</b> in the Passive Avoidance Test and the Formalin Test. While compound <b>6</b> did not show a statistically significant influence on memory and learning, it showed analgesic properties in both acute (ED₅₀ = 20.9 mg/kg) and inflammatory (ED₅₀ = 17.5 mg/kg) pain.