Design and synthesis of thiophene dihydroisoquinolines as novel BACE1 inhibitors.
Bioorg Med Chem Lett
; 23(10): 3075-80, 2013 May 15.
Article
em En
| MEDLINE
| ID: mdl-23570791
ABSTRACT
Utilizing a structure based design approach, combined with extensive medicinal chemistry execution, highly selective, potent and novel BACE1 inhibitor 8 (BACE1 Alpha assay IC50=8nM) was made from a weak µM potency hit in an extremely efficient way. The detailed SAR and general design approaches will be discussed.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Inibidores de Proteases
/
Tiofenos
/
Desenho de Fármacos
/
Ácido Aspártico Endopeptidases
/
Secretases da Proteína Precursora do Amiloide
/
Isoquinolinas
Limite:
Humans
Idioma:
En
Revista:
Bioorg Med Chem Lett
Assunto da revista:
BIOQUIMICA
/
QUIMICA
Ano de publicação:
2013
Tipo de documento:
Article
País de afiliação:
Estados Unidos