TRPV1 modulators: structure-activity relationships using a rational combinatorial approach.
Bioorg Med Chem Lett
; 21(12): 3541-5, 2011 Jun 15.
Article
em En
| MEDLINE
| ID: mdl-21612926
ABSTRACT
A discrete library of linear and hydantoin-containing dipeptide derivatives, based on the Lys-Trp(Nps) scaffold, was prepared by solid-phase synthesis. SAR studies indicated that potency for TRPV1 blockade and selectivity towards NMDA is mainly dictated by the side-chain length and the basic nature of α, ω-groups in the N-terminal residue. The 2-Nps moiety at position 2 of Trp indole ring is preferred over the 2-pyridine one.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Canais de Cátion TRPV
/
Bibliotecas de Moléculas Pequenas
/
Anti-Inflamatórios
Limite:
Humans
Idioma:
En
Ano de publicação:
2011
Tipo de documento:
Article