1.
Bioorg Med Chem Lett
; 20(20): 6108-15, 2010 Oct 15.
Artigo
em Inglês
| MEDLINE
| ID: mdl-20833036
RESUMO
Resulting from a vHTS based on a pharmacophore alignment on known ß3-adrenoceptor ligands, an aryloxypropanolamine scaffold comprising a thienopyrimidine moiety was further optimized as a human ß3-AR agonist, yielding a lead compound with an excellent cellular activity of EC(50)=20 pM, selectivity over hß1- and hß2-adrenoceptors and a promising safety profile.
Assuntos
Antagonistas de Receptores Adrenérgicos beta 3/química , Antagonistas de Receptores Adrenérgicos beta 3/farmacologia , Pirimidinas/química , Pirimidinas/farmacologia , Receptores Adrenérgicos beta 3/metabolismo , Antagonistas de Receptores Adrenérgicos beta 3/síntese química , Linhagem Celular , Sobrevivência Celular , Desenho de Fármacos , Humanos , Ligação Proteica , Pirimidinas/síntese química
2.
Bioorg Med Chem Lett
; 20(11): 3399-404, 2010 Jun 01.
Artigo
em Inglês
| MEDLINE
| ID: mdl-20434333
RESUMO
Using a vHTS based on a pharmacophore alignment on known beta3-adrenoceptor ligands, a set of intriguing beta-adrenoceptor ligands was identified, optimization of which resulted in a selective and potent human beta2-AR antagonist.