Lee, Jie Eun Koh, Hun Yeong Seo, Seon Hee Baek, Yi Yeon Rhim, Hyewhon Cho, Yong Seo Choo, Hyunah Pae, Ae Nim 2024-01-20T19:01:13Z 2024-01-20T19:01:13Z 2021-09-05 2010-07-15 0960-894X https://pubs.kist.re.kr/handle/201004/131250 T-type calcium channel is one of therapeutic targets for the treatment of cardiovascular diseases and neuropathic pain. In this study, as a part of our ongoing efforts to develop potent T-type calcium channel blockers, we designed oxazole derivatives substituted with arylpiperazinylalkylamines. The oxazoles were synthesized in a convenient convergent synthetic method, and biologically evaluated against alpha(1G) (Ca(V)3.1) T-type calcium channel. Among total 41 oxazole compounds synthesized, the most active one was the compound 10-35 with an IC(50) value of 0.65 mu M, which is comparable with that of mibefradil. (C) 2010 Elsevier Ltd. All rights reserved. English Pergamon Press Ltd. NEUROPATHIC PAIN CA2+ CHANNELS INHIBITION NEURONS Synthesis and biological evaluation of oxazole derivatives as T-type calcium channel blockers Article 10.1016/j.bmcl.2010.05.030 1 Bioorganic & Medicinal Chemistry Letters, v.20, no.14, pp.4219 - 4222 Bioorganic & Medicinal Chemistry Letters 20 14 4219 4222 scie scopus 000279258800051 2-s2.0-77953871878 Chemistry, Medicinal Chemistry, Organic Pharmacology & Pharmacy Chemistry Article NEUROPATHIC PAIN CA2+ CHANNELS INHIBITION NEURONS T-type calcium channel HTS assay alpha(1G) Subtype Neuropathic pain Oxazole