1.
Bioorg Med Chem Lett
; 13(10): 1729-32, 2003 May 19.
Artigo
em Inglês
| MEDLINE
| ID: mdl-12729652
RESUMO
Three series of spirocyclopiperazinium derivatives 5a-d, 6a-f and 17a-d were synthesized and evaluated for their in vivo analgesic activities. Compounds 5a, 17a and 17b exhibited excellent analgesic activity. Two important structure-activity relationships were observed from this study: (1) the quaternary ammonium functionality is a critical pharmacophore for analgesic activity; (2) it is important to adjust the lipophilic property of compounds to improve analgesic activity.