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4-(3-Aminoazetidin-1-yl)pyrimidin-2-amines as High-Affinity Non-imidazole Histamine H₃ Receptor Agonists with in Vivo Central Nervous System Activity.

ABSTRACT: Despite the high diversity of histamine H₃ receptor (H₃R) antagonist/inverse agonist structures, partial or full H₃R agonists have typically been imidazole derivatives. An in-house screening campaign intriguingly afforded the non-imidazole 4-(3-azetidin-1-yl)pyrimidin-2-amine 11b as a partial H₃R agonist. Here, the design, synthesis, and structure-activity relationships of 11b analogues are described. This series yields several non-imidazole full agonists with potencies varying with the alkyl substitution pattern on the basic amine following the in vitro evaluation of H₃R agonism using a cyclic adenosine monophosphate response element-luciferase reporter gene assay. The key compound VUF16839 (14d) combines nanomola

SUBMITTER: Wagner G

PROVIDER: S-EPMC6912857 | biostudies-literature | 2019 Dec

REPOSITORIES: biostudies-literature

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4-(3-Aminoazetidin-1-yl)pyrimidin-2-amines as High-Affinity Non-imidazole Histamine H₃ Receptor Agonists with in Vivo Central Nervous System Activity.

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4-(3-Aminoazetidin-1-yl)pyrimidin-2-amines as High-Affinity Non-imidazole Histamine H3 Receptor Agonists with in Vivo Central Nervous System Activity.

OmicsDI is part of the ELIXIR infrastructure

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4-(3-Aminoazetidin-1-yl)pyrimidin-2-amines as High-Affinity Non-imidazole Histamine H₃ Receptor Agonists with in Vivo Central Nervous System Activity.