Discovery of betrixaban (PRT054021), N-(5-chloropyridin-2-yl)-2-(4-(N, N-dimethylcarbamimidoyl) benzamido)-5-methoxybenzamide, a highly potent, selective, and …

…, T Su, J Fan, Y Wu, W Li, J Woolfrey, U Sinha…

文献索引：Zhang, Penglie; Huang, Wenrong; Wang, Lingyan; Bao, Liang; Jia, Zhaozhong J.; Bauer, Shawn M.; Goldman, Erick A.; Probst, Gary D.; Song, Yonghong; Su, Ting; Fan, Jingmei; Wu, Yanhong; Li, Wenhao; Woolfrey, John; Sinha, Uma; Wong, Paul W.; Edwards, Susan T.; Arfsten, Ann E.; Clizbe, Lane A.; Kanter, James; Pandey, Anjali; Park, Gary; Hutchaleelaha, Athiwat; Lambing, Joseph L.; Hollenbach, Stanley J.; Scarborough, Robert M.; Zhu, Bing-Yan Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 8 p. 2179 - 2185

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被引用次数: 52

摘要

Systematic SAR studies of in vitro factor Xa inhibitory activity around compound 1 were performed by modifying each of the three phenyl rings. A class of highly potent, selective, efficacious and orally bioavailable direct factor Xa inhibitors was discovered. These compounds were screened in hERG binding assays to examine the effects of substitution groups on the hERG channel affinity. From the leading compounds, betrixaban ( ...