Discovery of 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid diamides that increase CFTR mediated chloride transport.
Bioorg Med Chem Lett
; 15(8): 2087-91, 2005 Apr 15.
Article
em En
| MEDLINE
| ID: mdl-15808474
ABSTRACT
A series of 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid diamides that increase chloride transport in cells expressing mutant cystic fibrosis transmembrane conductance regulator (CFTR) protein has been identified from our compound library. Analoging efforts and the resulting structure-activity relationships uncovered are detailed. Compound potency was improved over 30-fold from the original lead, yielding several analogs with EC(50) values below 10nM in our cellular chloride transport assay.
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Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Cloretos
/
Regulador de Condutância Transmembrana em Fibrose Cística
/
Tetra-Hidroisoquinolinas
/
Amidas
Limite:
Animals
Idioma:
En
Revista:
Bioorg Med Chem Lett
Assunto da revista:
BIOQUIMICA
/
QUIMICA
Ano de publicação:
2005
Tipo de documento:
Article