新型3-羧酰胺基香豆素作为强效和选择性FXIIa抑制剂。
Novel 3-carboxamide-coumarins as potent and selective FXIIa inhibitors.
作者信息
Robert Séverine, Bertolla Carine, Masereel Bernard, Dogné Jean-Michel, Pochet Lionel
机构信息
Department of Pharmacy, Drug Design and Discovery Center, FUNDP, University of Namur, Namur, Belgium.
出版信息
J Med Chem. 2008 Jun 12;51(11):3077-80. doi: 10.1021/jm8002697. Epub 2008 May 7.
PMID:18459730
Abstract
Recently, FXIIa was highlighted as an original attractive target for the development of new anticoagulant drugs with low rates of therapy-related hemorrhages. In this work, we describe the development of a new series of 3-carboxamide-coumarins that are the first potent and selective nonpeptidic inhibitors of FXIIa.
摘要
最近，FXIIa作为开发治疗相关出血率低的新型抗凝药物的一个极具吸引力的原始靶点而备受关注。在这项研究中，我们描述了一系列新型3-羧酰胺香豆素的开发情况，这些香豆素是首批强效且具有选择性的FXIIa非肽类抑制剂。
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