60013-09-4Relevant academic research and scientific papers
Unique spirocyclopiperazinium salt. Part 2: Synthesis and structure-activity relationship of dispirocyclopiperazinium salts as analgesics
Wang, Xin,Gao, Feng-Li,Piao, Hong-Bin,Cheng, Tie-Ming,Li, Run-Tao
, p. 1729 - 1732 (2007/10/03)
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.
