1.
Discovery of a novel, potent and orally active series of gamma-lactams as selective NK1 antagonists.
Bioorg Med Chem Lett
; 18(14): 4168-71, 2008 Jul 15.
Artigo
em Inglês
| MEDLINE
| ID: mdl-18547807
RESUMO
Strategic replacement of the nitrogen of the lead compound 1 in the original cyclic urea series with a carbon resulted in the discovery of a novel, potent and orally more efficacious gamma-lactam series of selective NK(1) antagonists. Optimization of the lactam series culminated in the identification of compounds with high binding affinity and excellent oral CNS activity.
Assuntos
Lactamas/química , Antagonistas dos Receptores de Neurocinina-1 , Receptores da Neurocinina-1/química , Administração Oral , Química Farmacêutica/métodos , Desenho de Fármacos , Humanos , Modelos Químicos , Estrutura Molecular , Nitrogênio/química , Ligação Proteica , Relação Estrutura-Atividade , Substância P/química , Ureia/química , Vômito
2.
Org Lett
; 5(23): 4249-51, 2003 Nov 13.
Artigo
em Inglês
| MEDLINE
| ID: mdl-14601972
RESUMO
[structure: see text] A highly efficient and practical synthesis of 4,4-Disubstituted-2-Imidazolidinones utilizing a "self-reproduction of the center of chirality" strategy is described.