II. SAR studies of pyridyl-piperazinyl-piperidine derivatives as CXCR3 chemokine antagonists.
Bioorg Med Chem Lett
; 21(5): 1527-31, 2011 Mar 01.
Article
em En
| MEDLINE
| ID: mdl-21277198
ABSTRACT
The structure-human CXCR3 binding affinity relationship of a series of pyridyl-piperazinyl-piperidine derivatives was explored. The optimization campaign highlighted the pronounced effect of 2'-piperazine substitution on CXCR3 receptor affinity. Analog 18j, harboring a 2'(S)-ethylpiperazine moiety, exhibited a human CXCR3 IC(50) of 0.2 nM.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Piperazinas
/
Piperidinas
/
Piridinas
/
Receptores CXCR3
Idioma:
En
Ano de publicação:
2011
Tipo de documento:
Article