1.
Bioorg Med Chem Lett
; 30(15): 127279, 2020 08 01.
Artigo
em Inglês
| MEDLINE
| ID: mdl-32527459
RESUMO
The synthesis and structure activity relationship development of a pyrimidine series of heterocyclic Factor IXa inhibitors is described. Increased selectivity over Factor Xa inhibition was achieved through SAR expansion of the P1 element. Select compounds were evaluated in vivo to assess their plasma levels in rat.
Assuntos
Descoberta de Drogas , Fator IXa/antagonistas & inibidores , Inibidores do Fator Xa/farmacologia , Pirimidinas/farmacologia , Relação Dose-Resposta a Droga , Fator IXa/metabolismo , Inibidores do Fator Xa/síntese química , Inibidores do Fator Xa/química , Humanos , Estrutura Molecular , Pirimidinas/síntese química , Pirimidinas/química , Relação Estrutura-Atividade
2.
Bioorg Med Chem Lett
; 20(3): 1278-83, 2010 Feb 01.
Artigo
em Inglês
| MEDLINE
| ID: mdl-20018510
RESUMO
The syntheses and SAR investigations of novel CB(1) receptor antagonists based on a 1,2-diaryl piperidine core have been described. Optimization of this core afforded a compound with robust in vivo potency by reducing food intake in a mouse DIO model.
