探索一系列新型 PAR1 拮抗剂。
Exploration of a new series of PAR1 antagonists.
机构信息
Department of Medicinal Chemistry 4, Centre de Recherche Pierre Fabre, 17 Avenue Jean Moulin, 81106 Castres Cedex, France.
出版信息
Bioorg Med Chem Lett. 2010 Mar 1;20(5):1735-9. doi: 10.1016/j.bmcl.2010.01.050. Epub 2010 Jan 20.
Two series of new PAR1 antagonists have been identified. The first incorporates a cinnamoylpiperidine motif and the second a cinnamoylpyridine pattern. The synthesis, biological activity and structure-activity relationship of these compounds are presented. In each series, one analog showed potent in vivo antithrombotic activity in a rat AV shunt model, with up to 53% inhibition at 1.25mpk iv for compound 30.
已经鉴定出了两类新的 PAR1 拮抗剂。第一类包含一个肉桂酰哌啶基序，第二类包含一个肉桂酰吡啶模式。介绍了这些化合物的合成、生物活性和构效关系。在每个系列中，一种类似物在大鼠动静脉分流模型中显示出强大的体内抗血栓活性，化合物 30 在 1.25mpk iv 时的抑制率高达 53%。
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