Novel L-prolyl-L-leucylglycinamide (PLG) tripeptidomimetics based on a 2-azanorbornane scaffold as positive allosteric modulators of the D2R

• Tipo: Artigo em Revista Científica Internacional
• Data: 2016

Autores

Sampaio Dias, IE (Autor) Outra; Sousa, CAD (Autor) Outra; Garcia Mera, X (Autor) Outra; da Costa, JF (Autor) Outra; Caamano, O (Autor) Outra; Rodriguez Borges, JE (Autor) FCUP

Revista

Título: Organic and Biomolecular Chemistry

Vol. 14

Páginas: 11065-11069

ISSN: 1477-0520

Editora: Royal Society of Chemistry

Indexação

ISI Web of Knowledge - 12 Citações

Scopus - 12 Citações

Outras Informações

ID Authenticus: P-00M-B4W

DOI: 10.1039/c6ob02248k

Abstract (EN): An efficient and straightforward orthogonal methodology was successfully developed to achieve constrained L-prolyl-L-leucylglycinamide (PLG) analogues starting from two proline mimetics based on a 2-azanorbornane scaffold. A preliminary dopamine D-2 receptor radiolabeled binding assay with [H-3]-N-propylnorapomorphine shows that enantiopurity of PLG peptidomimetics based on 2-azanorbornane is a requirement to achieve statistically significant positive modulators of the D-2 receptor. This is the first documented active peptidomimetic of PLG whose bioactivity is not correlated with the C-terminal carboxamide pharmacophore and which cannot adopt the hypothesized type II beta-turn conformation.

Idioma: Inglês

Tipo (Avaliação Docente): Científica

Nº de páginas: 5