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新型T型钙通道阻滞剂：二氧喹唑啉甲酰胺衍生物。

Novel T-type calcium channel blockers: dioxoquinazoline carboxamide derivatives.

作者信息

Jo Mi Na, Seo Hee Jeong, Kim Yoonji, Seo Seon Hee, Rhim Hyewhon, Cho Yong Seo, Cha Joo Hwan, Koh Hun Yeong, Choo Hyunah, Pae Ae Nim

机构信息

Life Sciences Division, Korea Institute of Science and Technology, PO Box 131, Cheongryang, Seoul 130-650, Republic of Korea.

出版信息

Bioorg Med Chem. 2007 Jan 1;15(1):365-73. doi: 10.1016/j.bmc.2006.09.051. Epub 2006 Oct 10.

DOI:10.1016/j.bmc.2006.09.051
PMID:17035033
Abstract

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 1n shows the most potent T-type calcium current blocking activity with an IC(50) value of 1.52 microM, which is comparable to that of mibefradil.

摘要

T型钙通道是治疗心血管疾病和神经性疼痛的治疗靶点之一。自从T型钙通道阻滞剂米贝拉地尔撤市以来，人们为开发T型钙通道阻滞剂付出了诸多努力。设计、合成了一个包含155种化合物的二氧喹唑啉甲酰胺衍生物小分子文库，并对其进行了T型钙通道阻断活性的生物学评估。在合成的那些化合物中，化合物1n表现出最有效的T型钙电流阻断活性，IC(50)值为1.52微摩尔，与米贝拉地尔相当。

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