Jo, Mi Na Seo, Hee Jeong Kim, Yoonji Seo, n Hee Seo Rhim, Hyewhon Cho, Yong Seo Cha, Joo Hwan Koh, Hun Yeong Choo, Hyunah Pae, Ae Nim 2024-01-21T01:34:59Z 2024-01-21T01:34:59Z 2021-09-05 2007-01-01 0968-0896 https://pubs.kist.re.kr/handle/201004/134749 T-type calcium channel is one of therapeutic targets for the treatment of cardiovascular diseases and neuropathic pains. Since the withdrawal of mibefradil, a T-type calcium channel blocker, there have been a lot of efforts to develop T-type calcium channel blockers. A small molecule library of dioxoquinazoline carboxamide derivatives containing 155 compounds was designed, synthesized, and biologically evaluated for T-type calcium channel blocking activity. Among those compounds synthesized, the compound In shows the most potent T-type calcium current blocking activity with an IC50 value of 1.52 mu M, which is comparable to that of mibefradil. (c) 2006 Elsevier Ltd. All rights reserved. English PERGAMON-ELSEVIER SCIENCE LTD BIOLOGICAL EVALUATION CA2+ CHANNELS Novel T-type calcium channel blockers: Dioxoquinazoline carboxamide derivatives Article 10.1016/j.bmc.2006.09.051 1 BIOORGANIC & MEDICINAL CHEMISTRY, v.15, no.1, pp.365 - 373 BIOORGANIC & MEDICINAL CHEMISTRY 15 1 365 373 scie scopus 000243087200035 2-s2.0-33750952104 Biochemistry & Molecular Biology Chemistry, Medicinal Chemistry, Organic Biochemistry & Molecular Biology Pharmacology & Pharmacy Chemistry Article BIOLOGICAL EVALUATION CA2+ CHANNELS T-type calcium channel blockers dioxoquinazoline carboxamide derivatives