发现二苯并内酰胺衍生物作为 N 型钙通道阻滞剂。
Discovery of diphenyl lactam derivatives as N-type calcium channel blockers.
机构信息
Abbott Laboratories, Global Pharmaceutical Research and Development, Abbott Park, IL 60064, USA.
出版信息
Bioorg Med Chem Lett. 2012 Feb 15;22(4):1716-8. doi: 10.1016/j.bmcl.2011.12.100. Epub 2012 Jan 8.
PMID:22277280
Abstract
A novel series of diphenyl lactam containing calcium channel blockers is described. Extensive SAR studies resulted in compounds with low molar activity and good plasma exposure after oral dosing. Compounds 2, 6 and 7 demonstrated significant efficacy in the capsaicin model of secondary hyperalgesia following oral administration.
摘要
描述了一系列新型含二苯甲酰基内酰胺的钙通道阻滞剂。广泛的 SAR 研究得到了摩尔活性低且口服给药后具有良好血浆暴露的化合物。化合物 2、6 和 7 在口服后辣椒素诱导的继发性痛觉过敏模型中表现出显著的疗效。
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