1.
Bioorg Med Chem Lett
; 12(21): 3073-6, 2002 Nov 04.
Artigo
em Inglês
| MEDLINE
| ID: mdl-12372504
RESUMO
The combination of a 3,5-bis(trifluoromethyl)phenyl needle with the spiropyrrolo-pyrrole motive as a privileged GPCR scaffold was the basis for designing a focused combinatorial library targeted towards the neurokinin-1 receptor. A solution- and solid-phase method is described and binding affinities of representative compounds are presented.
Assuntos
Pirróis/síntese química , Pirróis/farmacologia , Receptores da Neurocinina-1/metabolismo , Receptores da Neurocinina-2/metabolismo , Receptores da Neurocinina-3/metabolismo , Técnicas de Química Combinatória , Proteínas de Ligação ao GTP/metabolismo , Indicadores e Reagentes , Ligantes , Receptores da Neurocinina-1/efeitos dos fármacos , Receptores da Neurocinina-2/efeitos dos fármacos , Receptores da Neurocinina-3/efeitos dos fármacos , Relação Estrutura-Atividade
2.
Bioorg Med Chem Lett
; 12(18): 2519-22, 2002 Sep 16.
Artigo
em Inglês
| MEDLINE
| ID: mdl-12182851
RESUMO
The combination of the 3,5-bis(trifluoromethyl)phenyl group with a spirohydantoin motive as a central scaffold was the basis for the design of a combinatorial library targeted towards the neurokinin-1 receptor. A solution- and solid-phase procedure is described and binding affinities of representative compounds presented.