1.
Chem Pharm Bull (Tokyo)
; 57(3): 288-93, 2009 Mar.
Artigo
em Inglês
| MEDLINE
| ID: mdl-19252322
RESUMO
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.
Assuntos
Diaminas/síntese química , Antagonistas dos Receptores Histamínicos H3/síntese química , Imidazolidinas/química , Nitrilas/química , Receptores Histamínicos H3/metabolismo , Animais , Diaminas/química , Diaminas/farmacologia , Antagonistas dos Receptores Histamínicos H3/química , Antagonistas dos Receptores Histamínicos H3/farmacologia , Humanos , Imidazolidinas/síntese química , Concentração Inibidora 50 , Conformação Molecular , Nitrilas/síntese química , Ratos
2.
Bioorg Med Chem Lett
; 18(7): 2288-91, 2008 Apr 01.
Artigo
em Inglês
| MEDLINE
| ID: mdl-18353639
RESUMO
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.
