9-Dihydroerythromycins as non-antibiotic motilin receptor agonists.
Bioorg Med Chem Lett
; 20(19): 5658-61, 2010 Oct 01.
Article
em En
| MEDLINE
| ID: mdl-20801039
ABSTRACT
A series of 9-dihydroerythromycin A and B analogues with modification of the desosamine nitrogen have been synthesized and screened for motilin agonist activity, antibiotic activity, tachyphylaxis and hERG channel current inhibition. Small alkyl groups resulted in the potency while compounds with a primary or secondary amine resulted in the low motilin agonist potency. Several compounds were identified as non-antibiotic motilin receptor agonists with minimal tachyphylaxis and low hERG interaction.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Receptores dos Hormônios Gastrointestinais
/
Eritromicina
/
Receptores de Neuropeptídeos
Limite:
Animals
Idioma:
En
Ano de publicação:
2010
Tipo de documento:
Article