Discovery of betrixaban (PRT054021), N-(5-chloropyridin-2-yl)-2-(4-(N,N-dimethylcarbamimidoyl)benzamido)-5-methoxybenzamide, a highly potent, selective, and orally efficacious factor Xa inhibitor.

@article{Zhang2009DiscoveryOB,
  title={Discovery of betrixaban (PRT054021), N-(5-chloropyridin-2-yl)-2-(4-(N,N-dimethylcarbamimidoyl)benzamido)-5-methoxybenzamide, a highly potent, selective, and orally efficacious factor Xa inhibitor.},
  author={Penglie Zhang and Wenrong Huang and Lingyan Wang and Liang Bao and Zhaozhong Jon Jia and Shawn M Bauer and Erick A Goldman and G. Duane Probst and Yonghong Song and Ting Su and Jingmei Fan and Yanhong Wu and Wenhao Li and John Woolfrey and Uma Sinha and Paul W. K. Wong and Susan T Edwards and Ann Elizabeth Arfsten and Lane A Clizbe and James Kanter and Anjali Pandey and Gary S Park and Athiwat Hutchaleelaha and Joseph L Lambing and Stanley J. Hollenbach and Robert Murry Scarborough and Bing-yan Zhu},
  journal={Bioorganic & medicinal chemistry letters},
  year={2009},
  volume={19 8},
  pages={2179-85}
}
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 (compound 11, PRT054021) has been selected as the clinical candidate… CONTINUE READING

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