Hong, Jin Ri Choo, Hyunah Nam, Ghilsoo 2024-01-20T00:33:12Z 2024-01-20T00:33:12Z 2021-09-05 2017-09-01 0960-894X https://pubs.kist.re.kr/handle/201004/122306 A novel series of arylsulfonylaminomethyl-3-(1-phenyl-5-isopropyl)pyrazoles was evaluated for serotonin receptor subtype 6 (5-HT6R) antagonistic effects in vitro. We also investigated their neuropathic pain-alleviating effects in vivo using a rat spinal nerve ligation (SNL) model. Bicyclic aromatic sulfonamino groups, such as naphthalene and quinolin-substituted derivatives, showed good 5-HT6 inhibitory activity in vitro. Among them, selected compounds, 12 and 13, having 8-quinoylsulfonamino groups, showed potent neuropathic pain-alleviating effects in the rat model. (C) 2017 Elsevier Ltd. All rights reserved. English Pergamon Press Ltd. ALZHEIMERS-DISEASE MEMORY RAT Neuropathic pain-alleviating effects of pyrazole-conjugated arylsulfonamides as 5-HT6 receptor antagonists Article 10.1016/j.bmcl.2017.07.031 1 Bioorganic & Medicinal Chemistry Letters, v.27, no.17, pp.4146 - 4149 Bioorganic & Medicinal Chemistry Letters 27 17 4146 4149 scie scopus 000410462500038 2-s2.0-85024094337 Chemistry, Medicinal Chemistry, Organic Pharmacology & Pharmacy Chemistry Article ALZHEIMERS-DISEASE MEMORY RAT Arylsulfonylaminomethylpyrazole Neuropathic pain 5-HT6 receptor antagonist