Optimization of the heterocyclic core of the quinazolinone-derived CXCR3 antagonists.
Bioorg Med Chem Lett
; 18(2): 688-93, 2008 Jan 15.
Article
em En
| MEDLINE
| ID: mdl-18061451
ABSTRACT
A series of six-six and six-five fused heterocyclic CXCR3 antagonists has been synthesized and their activities evaluated in an [(125)I]-IP-10 displacement assay and an ITAC mediated in vitro cell migration assay. The pharmacokinetic properties of several top compounds have also been studied. This effort led to the discovery of compounds with increased potency and improved pharmacokinetic properties that could serve as useful tools to study the role of the CXCR3 receptor in vivo.
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Base de dados:
MEDLINE
Assunto principal:
Quinazolinonas
/
Receptores CXCR3
/
Compostos Heterocíclicos
Limite:
Animals
/
Humans
Idioma:
En
Ano de publicação:
2008
Tipo de documento:
Article