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.
Tetrahedron
; 69(29): 5829-5840, 2013 Jul 22.
Artigo
em Inglês
| MEDLINE
| ID: mdl-23894213
RESUMO
The preparation of an indole appended vinamidinium salt, an indole appended vinylogous amide and an indole appended chloroenal are described. The subsequent regiospecific conversion of these indole containing building blocks to functionalized pyrazoles and pyrroles is detailed.