Synthesis and the 5-HT6 receptor antagonistic effect of 3-arylsulfonylamino-5,6-dihydro-6-substituted pyrazolo[3,4]pyridinones for neuropathic pain treatment

Authors
Devegowda, Vani NelamaneHong, Jin-RiCho, SungjinLim, Eun JeongChoo, HyunahKeum, GyochangRhim, HyewonNam, Ghilsoo
Issue Date
2013-08-15
Publisher
Pergamon Press Ltd.
Citation
Bioorganic & Medicinal Chemistry Letters, v.23, no.16, pp.4696 - 4700
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. (C) 2013 Elsevier Ltd. All rights reserved.
Keywords
SEROTONIN; DERIVATIVES; BINDING; MODEL; SEROTONIN; DERIVATIVES; BINDING; MODEL; Arylsufonylamino-5,6-dihydro-pyrazolo[3,4-c]pyridine-7-one; Synthesis; 5-HT6 receptor antagonist; Neuropathic pain
ISSN
0960-894X
URI
https://pubs.kist.re.kr/handle/201004/127769
DOI
10.1016/j.bmcl.2013.05.100
Appears in Collections:
KIST Article > 2013
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