P3 cap modified Phe*-Ala series BACE inhibitors.
Bioorg Med Chem Lett
; 14(1): 245-50, 2004 Jan 05.
Article
em En
| MEDLINE
| ID: mdl-14684336
ABSTRACT
With the aim of reducing molecular weight and adjusting log D value of BACE inhibitors to more favorable range for BBB penetration and better bioavailability, we synthesized and evaluated several series of P3 cap modified BACE inhibitors obtained via replacement of the P3NHBoc moiety as seen in 3 with other polar functional groups such as amino, hydroxyl and fluorine. Several promising inhibitors emerging from this P3 cap SAR study (e.g., 15 and 19) demonstrated good enzyme inhibitory potencies (BACE-1 IC(50) <50 nM) and whole cell activities (IC(50) approximately 1 microM).
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Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Endopeptidases
/
Inibidores de Proteases
/
Dipeptídeos
Limite:
Humans
Idioma:
En
Ano de publicação:
2004
Tipo de documento:
Article