Novel GlyT1 inhibitor chemotypes by scaffold hopping. Part 2: development of a [3.3.0]-based series and other piperidine bioisosteres.
Bioorg Med Chem Lett
; 24(4): 1062-6, 2014 02 15.
Article
em En
| MEDLINE
| ID: mdl-24462664
ABSTRACT
This Letter describes the development and SAR of a novel series of GlyT1 inhibitors derived from a scaffold hopping approach, in lieu of an HTS campaign, which provided intellectual property position. Members within this new [3.3.0]-based series displayed excellent GlyT1 potency, selectivity, free fraction, and modest CNS penetration. Moreover, enantioselective GlyT1 inhibition was observed, within this novel series and a number of other piperidine bioisosteric cores.
Palavras-chave
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Piperidinas
/
Proteínas da Membrana Plasmática de Transporte de Glicina
Limite:
Humans
Idioma:
En
Revista:
Bioorg Med Chem Lett
Assunto da revista:
BIOQUIMICA
/
QUIMICA
Ano de publicação:
2014
Tipo de documento:
Article