Conformational restriction approach to BACE1 inhibitors II: SAR study of the isocytosine derivatives fixed with a cis-cyclopropane ring.
Bioorg Med Chem Lett
; 23(10): 2912-5, 2013 May 15.
Article
em En
| MEDLINE
| ID: mdl-23562056
ABSTRACT
To improve the efficacy of the conformationally restricted BACE1 inhibitors, structural modifications were investigated using two strategies (a) modification of the terminal aromatic ring and (b) insertion of a spacer between the aromatic rings. In the latter approach, another type of inhibitor 17 bearing an ethylene spacer between two aromatic rings was found to exhibit good BACE1 inhibitory activity, while the corresponding conformationally unrestricted compound 25 showed no activity. This result revealed an interesting effect of a conformational restriction with a cyclopropane ring.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Ácido Aspártico Endopeptidases
/
Ciclopropanos
/
Citosina
/
Inibidores Enzimáticos
/
Secretases da Proteína Precursora do Amiloide
Limite:
Humans
Idioma:
En
Ano de publicação:
2013
Tipo de documento:
Article