1.
Chem Pharm Bull (Tokyo)
; 57(3): 288-93, 2009 Mar.
Article
in English
| MEDLINE
| ID: mdl-19252322
ABSTRACT
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.
Subject(s)
Diamines/chemical synthesis , Histamine H3 Antagonists/chemical synthesis , Imidazolidines/chemistry , Nitriles/chemistry , Receptors, Histamine H3/metabolism , Animals , Diamines/chemistry , Diamines/pharmacology , Histamine H3 Antagonists/chemistry , Histamine H3 Antagonists/pharmacology , Humans , Imidazolidines/chemical synthesis , Inhibitory Concentration 50 , Molecular Conformation , Nitriles/chemical synthesis , Rats
2.
Bioorg Med Chem Lett
; 18(7): 2288-91, 2008 Apr 01.
Article
in English
| MEDLINE
| ID: mdl-18353639
ABSTRACT
Novel diamine derivatives containing imidazolidinylidene propanedinitrile were synthesized and evaluated for histamine H(3) receptor-binding affinities. High-affinity ligands 3d, 3k, and 3n showed potent H(3) receptor antagonism and excellent selectivity over human H(1), H(2) and H(4) receptors.
