5-Lipoxygenase-activating protein inhibitors. Part 2: 3-{5-((S)-1-Acetyl-2,3-dihydro-1H-indol-2-ylmethoxy)-3-tert-butylsulfanyl-1-[4-(5-methoxy-pyrimidin-2-yl)-benzyl]-1H-indol-2-yl}-2,2-dimethyl-propionic acid (AM679)--a potent FLAP inhibitor.
Bioorg Med Chem Lett
; 20(1): 213-7, 2010 Jan 01.
Article
em En
| MEDLINE
| ID: mdl-19914828
ABSTRACT
A series of potent 5-lipoxygenase-activating protein (FLAP) inhibitors are herein described. SAR studies focused on the discovery of novel alicyclic moieties appended to an indole core to optimize potency, physical properties and off-target activities. Subsequent SAR on the N-benzyl substituent of the indole led to the discovery of compound 39 (AM679) which showed potent inhibition of leukotrienes in human blood and in a rodent bronchoalvelolar lavage (BAL) challenge model.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Ácidos Pentanoicos
/
Proteínas de Transporte
/
Inibidores de Lipoxigenase
/
Indóis
/
Proteínas de Membrana
Limite:
Animals
/
Humans
Idioma:
En
Revista:
Bioorg Med Chem Lett
Ano de publicação:
2010
Tipo de documento:
Article