Diamine Derivatives Containing Imidazolidinylidene Propanedinitrile as a New Class of Histamine H_3 Receptor Antagonists : Conformationally Restricted Derivatives

概要

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Novel conformationally restricted diamine derivatives containing imidazolidinylidene propanedinitrile were synthesized and evaluated for human and rat histamine H_3 receptor (H_3R) binding affinities. Among them, compounds 2b, 2c, 2j, 2k and 2m were found to be potent ligands for both H_3Rs with K_i values in the sub-nanomolar range, and showed potent H_3 receptor antagonism.
公益社団法人日本薬学会の論文
2009-03-01