Structure activity relationship studies of tricyclic bispyran sulfone γ-secretase inhibitors.
Bioorg Med Chem Lett
; 23(3): 844-9, 2013 Feb 01.
Article
em En
| MEDLINE
| ID: mdl-23265892
ABSTRACT
An investigation is detailed of the structure activity relationships (SAR) of two sulfone side chains of compound (-)-1a (SCH 900229), a potent, PS1-selective γ-secretase inhibitor and clinical candidate for the treatment of Alzheimer's disease. Specifically, 4-CF(3) and 4-Br substituted arylsulfone analogs, (-)-1b and (-)-1c, are equipotent to compound (-)-1a. On the right hand side chain, linker size and terminal substituents of the pendant sulfone group are also investigated.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Sulfonas
/
Benzopiranos
/
Inibidores Enzimáticos
/
Secretases da Proteína Precursora do Amiloide
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