Novel dihydropyrazine analogues as NPY antagonists.
Bioorg Med Chem Lett
; 12(3): 337-40, 2002 Feb 11.
Article
en En
| MEDLINE
| ID: mdl-11814791
ABSTRACT
The dihydropyridine is currently one of the lead compounds in the neuropeptide-Y(1) (NPY-Y(1)) receptor antagonist program. Compound is a selective, high affinity ligand at the NPY-Y(1) receptors (IC(50)=4.2 nM) in SK-N-MC cells. To further expand the SAR study surrounding this dihydropyridine core structure we succeeded in synthesizing an analogous series of dihydropyrazine derivatives. This structural modification yielded compounds substantially different from the parent molecules in terms of molecular polarization and electron distribution while the overall molecular structure was generally preserved. This altered property should therefore provide us with additional SAR information on the optimal binding requirement with NPY receptors.
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Base de datos:
MEDLINE
Asunto principal:
Pirazinas
/
Neuropéptido Y
Idioma:
En
Revista:
Bioorg Med Chem Lett
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2002
Tipo del documento:
Article