1.
Bioorg Med Chem Lett
; 18(18): 4936-9, 2008 Sep 15.
Artigo
em Inglês
| MEDLINE
| ID: mdl-18768319
RESUMO
High throughput screening of our compound collection led to the discovery of a novel series of N-alkyl-5H-pyrido[4,3-b]indol-1-amines as urotensin-II receptor antagonists. Synthesis, initial structure and activity relationships, functional and animal ortholog activities of the series are described.
Assuntos
Aminas/síntese química , Aminas/farmacologia , Piridinas/síntese química , Piridinas/farmacologia , Urotensinas/antagonistas & inibidores , Aminas/química , Animais , Técnicas de Química Combinatória , Camundongos , Estrutura Molecular , Piridinas/química , Relação Estrutura-Atividade
2.
Bioorg Med Chem Lett
; 18(9): 2860-4, 2008 May 01.
Artigo
em Inglês
| MEDLINE
| ID: mdl-18420409
RESUMO
A series of 2-aminomethyl piperidines has been discovered as novel urotensin-II receptor antagonists. The synthesis, initial structure-activity relationships, and optimization of the initial hit that resulted in the identification of potent, cross-species active, and functional urotensin-II receptor antagonists such as 1a and 11a are described.