Cyclic hydroxyamidines as amide isosteres: discovery of oxadiazolines and oxadiazines as potent and highly efficacious γ-secretase modulators in vivo.
J Med Chem
; 55(1): 489-502, 2012 Jan 12.
Article
em En
| MEDLINE
| ID: mdl-22098494
ABSTRACT
Cyclic hydroxyamidines were designed and validated as isosteric replacements of the amide functionality. Compounds with these structural motifs were found to be metabolically stable and to possess highly desirable pharmacokinetic profiles. These designs were applied in the identification of γ-secretase modulators leading to highly efficacious agents for reduction of central nervous system Aß(42) in various animal models.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Oxidiazóis
/
Oxazinas
/
Secretases da Proteína Precursora do Amiloide
/
Amidinas
Idioma:
En
Ano de publicação:
2012
Tipo de documento:
Article