288309-84-2Relevant academic research and scientific papers
Design and synthesis of factor Xa inhibitors and their prodrugs
Song, Yonghong,Clizbe, Lane,Bhakta, Chhaya,Teng, Willy,Wong, Paul,Huang, Brian,Tran, Katherine,Sinha, Uma,Park, Gary,Reed, Andrea,Scarborough, Robert M.,Zhu, Bing-Yan
, p. 297 - 300 (2007/10/03)
In addition to our previously reported fluoro acrylamides Xa inhibitors 2 and 3, a series of potent and novel cyclic diimide amidine compounds has been identified. In efforts to improve their oral bioavailability, replacement of the amidine group with methyl amidrazone gives compounds of moderate potency (14, IC50=0.028 μM). In the amidoxime prodrug approach, the amidoxime compounds show good oral bioavailability in rats and dogs. High plasma level of prodrug 26 and significant concentration of active drug 26a were obtained upon oral administration of prodrug 26 in rats.
Inhibitors of factor Xa
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, (2008/06/13)
Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating coagulation disorders.
Design, synthesis, and SAR of substituted acrylamides as factor Xa inhibitors.
Song, Yonghong,Clizbe, Lane,Bhakta, Chhaya,Teng, Willy,Li, Wenhao,Wu, Yanhong,Jia, Zhaozhong Jon,Zhang, Penglie,Wang, Lingyan,Doughan, Brandon,Su, Ting,Kanter, James,Woolfrey, John,Wong, Paul,Huang, Brian,Tran, Katherine,Sinha, Uma,Park, Gary,Reed, Andrea,Malinowski, John,Hollenbach, Stan,Scarborough, Robert M,Zhu, Bing-Yan
, p. 1511 - 1515 (2007/10/03)
Substituted acrylamides were used as templates that bridge P1 and P4 binding elements, resulting in a series of potent (sub-nanomolar) and selective factor Xa inhibitors. In this template, cis-geometry of P1 and P4 ligands is highly preferred. SAR on the substituting groups, as well as on modification of P1 and P4 moieties is described. Compounds in this series show good in vivo efficacy in animal models.
