Unique spirocyclopiperazinium salt. Part 2: synthesis and structure-activity relationship of dispirocyclopiperazinium salts as analgesics.
Basic Information
ID: ALA1136387
Journal: Bioorg Med Chem Lett
Title: Unique spirocyclopiperazinium salt. Part 2: synthesis and structure-activity relationship of dispirocyclopiperazinium salts as analgesics.
Authors: Wang X, Gao FL, Piao HB, Cheng TM, Li RT.
Abstract: 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.
CiteXplore: 12729652
DOI: 10.1016/s0960-894x(03)00213-0
Patent ID: ┄