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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 H-3 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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