4-Oxypiperidine Ethers as Multiple Targeting Ligands at Histamine H3 Receptors and Cholinesterases
Beata Michalska,
Marek Dzięgielewski,
Justyna Godyń
et al.
Abstract:This study examines the properties of a novel series of 4-oxypiperidines designed and synthesized as histamine H 3 R antagonists/inverse agonists based on the structural modification of two lead compounds, viz., ADS003 and ADS009. The products are intended to maintain a high affinity for H 3 R while simultaneously inhibiting AChE or/and BuChE enzymes. Selected compounds were subjected to hH 3 R radioligand displacement and gpH 3 R functional assays. Some of the compounds showed nanomolar affinity. The most pro… Show more
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