Synthesis and the 5-HT6 receptor antagonistic effect of 3-arylsulfonylamino-5,6-dihydro-6-substituted pyrazolo[3,4]pyridinones for neuropathic pain treatment
- Synthesis and the 5-HT6 receptor antagonistic effect of 3-arylsulfonylamino-5,6-dihydro-6-substituted pyrazolo[3,4]pyridinones for neuropathic pain treatment
- 와니; 홍진리; 조성진; 임은정; 추현아; 금교창; 임혜원; 남길수
- 5-HT6 receptor; neuropathic pain; antagonist; pyrazolopuridinone; serotonin; 5-HT6 receptor antagonist; arylsulfonylamino-5,6-dihydro-pyrazolo[3,4-c]pyrid; Synthesis
- Issue Date
- Bioorganic & medicinal chemistry letters
- VOL 23, NO 16, 4696-4700
- 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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