Devegowda, Vani Nelamane Hong, Jin-Ri Cho, Sungjin Lim, Eun Jeong Choo, Hyunah Keum, Gyochang Rhim, Hyewon Nam, Ghilsoo 2024-01-20T11:34:47Z 2024-01-20T11:34:47Z 2021-09-05 2013-08-15 0960-894X https://pubs.kist.re.kr/handle/201004/127769 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. English Pergamon Press Ltd. SEROTONIN DERIVATIVES BINDING MODEL Synthesis and the 5-HT6 receptor antagonistic effect of 3-arylsulfonylamino-5,6-dihydro-6-substituted pyrazolo[3,4]pyridinones for neuropathic pain treatment Article 10.1016/j.bmcl.2013.05.100 1 Bioorganic & Medicinal Chemistry Letters, v.23, no.16, pp.4696 - 4700 Bioorganic & Medicinal Chemistry Letters 23 16 4696 4700 scie scopus 000322611900040 2-s2.0-84880601634 Chemistry, Medicinal Chemistry, Organic Pharmacology & Pharmacy Chemistry Article SEROTONIN DERIVATIVES BINDING MODEL Arylsufonylamino-5,6-dihydro-pyrazolo[3,4-c]pyridine-7-one Synthesis 5-HT6 receptor antagonist Neuropathic pain