Fluorinated non-imidazole histamine H3 receptor antagonists

Fluorine substituents have become a widespread and important component in drug design and development. Here, the synthesis of fluorine containing compounds and some corresponding precursor molecules are presented for potential isotope labelling as well as their data obtained with in vitro and in vivo screenings. The compounds vary in the basic centres (piperidine or pyrrolidine) and are fluoro substituted in different positions of the basic alicyclic moiety. Pharmacological evaluation resulted in ligands with high affinities at hH3 receptor in the nanomolar and subnanomolar concentration range and some with high antagonist in vivo potencies.

Novel dibasic fluorinated non-imidazole histamine H3 receptor antagonists were prepared with high affinities at hH3 receptor in the nanomolar and subnanomolar concentration range and some with high antagonist in vivo potencies.Figure optionsDownload as PowerPoint slide