Diamine Derivatives Containing Imidazolidinylidene Propanedinitrile as a New Class of Histamine H3 Receptor Antagonists: Conformationally Restricted Derivatives

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Diamine derivatives containing imidazolidinylidene propanedinitrile as a new class of histamine H(3) receptor antagonists: conformationally restricted derivatives.

Novel conformationally restricted diamine derivatives containing imidazolidinylidene propanedinitrile were synthesized and evaluated for human and rat histamine H(3) receptor (H(3)R) binding affinities. Among them, compounds 2b, 2c, 2j, 2k and 2m were found to be potent ligands for both H(3)Rs with K(i) values in the sub-nanomolar range, and showed potent H(3) receptor antagonism.

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ژورنال

عنوان ژورنال: Chemical and Pharmaceutical Bulletin

سال: 2009

ISSN: 0009-2363,1347-5223

DOI: 10.1248/cpb.57.288