The discovery of small molecule inhibitors of neutral endopeptidase. Structure-activity studies on functionalized glutaramides.
Chem Biol Drug Des
; 67(1): 74-7, 2006 Jan.
Article
en En
| MEDLINE
| ID: mdl-16492151
ABSTRACT
A series of small molecule glutaramides were synthesized and evaluated for potency against canine and human neutral endopeptidase using target criteria of molecular weight <400 and log P between 2 and 4.5 to maximize the likelihood of achieving good oral absorption. The structure-activity relationship (SAR) investigations described in this paper led to the identification of an ethyl 1,3,4-thiadiazole glutaramide which demonstrated good neutral endopeptidase potency, selectivity and excellent oral absorption in the rat.
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Banco de datos:
MEDLINE
Asunto principal:
Ácidos Pentanoicos
/
Tiadiazoles
/
Inhibidores Enzimáticos
/
Amidas
Tipo de estudio:
Prognostic_studies
Límite:
Animals
/
Female
/
Humans
Idioma:
En
Año:
2006
Tipo del documento:
Article