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Structural modifications in the distal, regulatory region of histamine H3 receptor antagonists leading to the identification of a potent anti-obesity agent

Szczepańska, Katarzyna ; Pockes, Steffen ; Podlewska, Sabina ; Höring, Carina ; Mika, Kamil ; Latacz, Gniewomir ; Bednarski, Marek ; Siwek, Agata ; Karcz, Tadeusz ; Nagl, Martin ; Bresinsky, Merlin ; Mönnich, Denise ; Seibel, Ulla ; Kuder, Kamil J. ; Kotańska, Magdalena ; Stark, Holger ; Elz, Sigurd ; Kieć-Kononowicz, Katarzyna


A series of 4-pyridylpiperazine derivatives with varying regulatory region substituents proved to be potent histamine H3 receptor (H3R) ligands in the nanomolar concentration range. The most influential modification that affected the affinity toward the H3R appeared by introducing electron-withdrawing moieties into the distal aromatic ring. In order to finally discuss the influence of the ...


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