1.
Bioorg Med Chem Lett
; 12(19): 2719-22, 2002 Oct 07.
Artigo
em Inglês
| MEDLINE
| ID: mdl-12217362
RESUMO
A series of novel spiroether-based neurokinin-1 (NK(1)) antagonists is described. The effect of modifications to the spiroether ring and aromatic substituents are discussed, leading to the identification of compounds with high affinity and excellent CNS penetration.
Assuntos
Éteres/síntese química , Éteres/farmacologia , Antagonistas dos Receptores de Neurocinina-1 , Compostos de Espiro/síntese química , Compostos de Espiro/farmacologia , Animais , Antieméticos/síntese química , Antieméticos/farmacologia , Comportamento Animal/efeitos dos fármacos , Ligação Competitiva/efeitos dos fármacos , Células CHO , Cricetinae , Cães , Furões , Gerbillinae , Humanos , Ratos
2.
Bioorg Med Chem Lett
; 12(18): 2515-8, 2002 Sep 16.
Artigo
em Inglês
| MEDLINE
| ID: mdl-12182850
RESUMO
A series of novel spiroketal-based NK(1) antagonists is described. The effect of modifications to the spiroether ring and aromatic substituents are discussed, leading to the identification of compounds with high affinity and excellent CNS penetration.
