Peer-reviewed veterinary case report
Synthesis and the 5-HT6 receptor antagonistic effect of 3-arylsulfonylamino-5,6-dihydro-6-substituted pyrazolo[3,4]pyridinones for neuropathic pain treatment.
- Journal:
- Bioorganic & medicinal chemistry letters
- Year:
- 2013
- Authors:
- Devegowda, Vani Nelamane et al.
- Affiliation:
- Brain Science Institute · South Korea
- Species:
- rodent
Abstract
A novel series of 3-arylsulfonylamino-5,6-dihydro-6-substituted-1H-pyrazolo[3,4-c]pyridine-7-ones was designed and synthesized as 5-HT6 ligands. Among the derivatives synthesized, the lead compound, 12b, having piperidine functionality at the 6-position and (1-naphthyl)sulfonamino at the 3-position of the core structure showed the most potent 5-HT6 inhibitory activity in vitro, good stability without CYP liability, and good neuropathic pain alleviation activity in a rat animal model.
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Search related cases →Original publication: https://pubmed.ncbi.nlm.nih.gov/23820387/