| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1373235 | Bioorganic & Medicinal Chemistry Letters | 2007 | 5 Pages |
Abstract
Two novel classes of monospirocyclopiperazinium salts were designed, synthesized, and evaluated for their in vivo analgesic activities. Some interesting structure–activity relationships are revealed: (1) Spirocyclopiperazinium moiety is favorable to improve the analgesic activity; (2) The size and conformation of spirocyclopiperazinium moiety significantly affects the analgesic activity; (3) Phenylethyl group of 3d is a crucial pharmacophore. Among the compounds synthesized, 3d exhibited the most potent activity with low toxicity. Further antinociceptive mechanism studies of 3d showed that these compounds will be a new kind of analgesics.
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Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Qi Sun, Cai-Qin Yue, Jia Ye, Chang-Ling Li, Tie-Ming Cheng, Run-Tao Li,