Kim, Jung Hyun Keum, Gyochang Chung, Hesson Nam, Ghilsoo 2024-01-20T03:01:32Z 2024-01-20T03:01:32Z 2021-09-04 2016-11-10 0223-5234 https://pubs.kist.re.kr/handle/201004/123443 A novel series of aryl(1,5-disubstituted pyrazol-3-yl)methyl sulfonamide derivatives was designed, synthesized, and evaluated for T-type calcium channel (ctiG and chm) inhibitory activity. We identified several compounds, 9a, 9b, 9g, and 9h that displayed good T-type channel inhibitory potency with low hERG channel and CYP450 inhibition. Among them, 9a and 9b exhibited neuropathic pain alleviation effects in mechanical and cold allodynia induced in the SNL rat model. Compounds 9a and 9b displayed better efficacy than mibefradil and gabapentin against cold allodynia. In particular, compound 9a seemed to be valuable as shown fast acting performance in mechanical neuropathic pain model. (C) 2016 Elsevier Masson SAS. All rights reserved'. English ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER CA2+ CHANNELS PERIPHERAL NEUROPATHY RAT MODEL ZONISAMIDE ALLODYNIA BLOCKERS NEURONS Synthesis and T-type calcium channel-blocking effects of aryl(1,5-disubstituted-pyrazol-3-yl)methyl sulfonamides for neuropathic pain treatment Article 10.1016/j.ejmech.2016.07.032 1 EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, v.123, pp.665 - 672 EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 123 665 672 scie scopus 000385319000052 2-s2.0-84981711237 Chemistry, Medicinal Pharmacology & Pharmacy Article CA2+ CHANNELS PERIPHERAL NEUROPATHY RAT MODEL ZONISAMIDE ALLODYNIA BLOCKERS NEURONS T-type calcium channel inhibition Aryl(1,5-disubstituted-pyrazol-3-yl)methyl sulfonamide Neuropathic pain Allodynia