1.
Bioorg Med Chem Lett
; 18(8): 2640-4, 2008 Apr 15.
Artigo
em Inglês
| MEDLINE
| ID: mdl-18374566
RESUMO
2-Arylbenzoxazole 5 was identified as a hit from a fluorescence-based high-throughput screen for CETP inhibitors. The synthesis and SAR investigation employing array synthesis of the A- and B-rings are described.
Assuntos
Benzoxazóis/síntese química , Benzoxazóis/farmacologia , Proteínas de Transferência de Ésteres de Colesterol/antagonistas & inibidores , Benzoxazóis/química , Proteínas de Transferência de Ésteres de Colesterol/metabolismo , Humanos , Modelos Moleculares , Estrutura Molecular , Relação Estrutura-Atividade
2.
Bioorg Med Chem Lett
; 15(4): 1225-8, 2005 Feb 15.
Artigo
em Inglês
| MEDLINE
| ID: mdl-15686947
RESUMO
A structure-activity relationship study of the amine portion of the calcilytic compound NPS-2143 resulted in the discovery of substituted 2-benzylpyrrolidines as replacements for the 1,1-dimethyl-2-naphthalen-2-yl-ethylamine. When compared to NPS-2143, a newly discovered compound, 3h, exhibited similar potency as a calcium-sensing receptor (CaR) antagonist and a superior human ether-a-go-go related gene (hERG) profile.
