5-HT6 receptor antagonists. Design, synthesis, and structure–activity relationship of substituted 2-(1-methyl-4-piperazinyl)pyridines

Michał Gałęzowski, Charles-Henry Fabritius, Ullamari Pesonen, Harri Salo, Marta Olszak-Płachta, Klaudia Czerwińska, Justyna Adamczyk, Marcin Król,Peteris Prusis, Magdalena Sieprawska-Lupa, Maciej Mikulski, Katja Kuokkanen, Radosław Obuchowicz, Timo Korjamo, Niina Jalava,Agnieszka Nikiforuk,Mateusz Nowak

Bioorganic & Medicinal Chemistry Letters（2023）

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摘要

In this study, we present the discovery and pharmacological characterization of a new series of 6-piperazinyl-7-azaindoles. These compounds demonstrate potent antagonism and selectivity against the 5-HT6 receptor. Our research primarily focuses on optimizing the lead structure and investigating the structure–activity relationship (SAR) of these compounds. Our main objective is to improve their activity and selectivity against off-target receptors.

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关键词

Serotonin receptor,5-HT6 receptor,Antagonists,Pyridine core,Non-sulfonyl compounds

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