Design of an amide N-glycoside derivative of ß-glucogallin: a stable, potent, and specific inhibitor of aldose reductase.
J Med Chem
; 57(1): 71-7, 2014 Jan 09.
Article
em En
| MEDLINE
| ID: mdl-24341381
ABSTRACT
ß-Glucogallin (BGG), a major component of the Emblica officinalis medicinal plant, is a potent and selective inhibitor of aldose reductase (AKR1B1). New linkages (ether/triazole/amide) were introduced via high yielding, efficient syntheses to replace the labile ester, and an original two-step (90%) preparation of BGG was developed. Inhibition of AKR1B1was assessed in vitro and using transgenic lens organ cultures, which identified the amide linked glucoside (BGA) as a stable, potent, and selective therapeutic lead toward the treatment of diabetic eye disease.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Aldeído Redutase
/
Taninos Hidrolisáveis
/
Inibidores Enzimáticos
/
Amidas
/
Glicosídeos
Limite:
Humans
Idioma:
En
Revista:
J Med Chem
Ano de publicação:
2014
Tipo de documento:
Article