1.
Bioorg Med Chem Lett
; 18(14): 3848-51, 2008 Jul 15.
Artigo
em Inglês
| MEDLINE
| ID: mdl-18595695
RESUMO
A novel series of cyanoguanidine-piperazine P2X(7) antagonists were identified and structure-activity relationship (SAR) studies described. Compounds were assayed for activity at human and rat P2X(7) receptors in addition to their ability to inhibit IL-1 beta release from stimulated human whole blood cultures. Compound 27 possesses potent activity (0.12 microM) in this latter assay and demonstrates moderate clearance in-vivo.
