Literature DB >> 18424044

Structure-activity relationships of anthranilamide-based factor Xa inhibitors containing piperidinone and pyridinone P4 moieties.

James R Corte1, Tianan Fang, Donald J P Pinto, Wei Han, Zilun Hu, Xiang-Jun Jiang, Yun-Long Li, Jolicia F Gauuan, Mark Hadden, Darren Orton, Alan R Rendina, Joseph M Luettgen, Pancras C Wong, Kan He, Paul E Morin, Chong-Hwan Chang, Daniel L Cheney, Robert M Knabb, Ruth R Wexler, Patrick Y S Lam.   

Abstract

Introduction of the phenyl piperidinone and phenyl pyridinone P4 moieties in the anthranilamide scaffold led to potent, selective, and orally bioavailable inhibitors of factor Xa. Anthranilamide 28 displayed comparable efficacy to apixaban in the rabbit arteriovenous-shunt (AV) thrombosis model.

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Year:  2008        PMID: 18424044     DOI: 10.1016/j.bmcl.2008.03.092

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  5 in total

Review 1.  Structure-function relationships of factor Xa inhibitors: implications for the practicing clinician.

Authors:  Benjamin A Steinberg; Richard C Becker
Journal:  J Thromb Thrombolysis       Date:  2014       Impact factor: 2.300

2.  Exploration of conformational transition in the aryl-binding site of human FXa using molecular dynamics simulations.

Authors:  Jing-Fang Wang; Pei Hao; Yi-Xue Li; Jian-Liang Dai; Xuan Li
Journal:  J Mol Model       Date:  2011-11-25       Impact factor: 1.810

3.  Efficient one-pot protocol for diverse pyrazolylphosphonates by multi-component reactions: their antioxidant and antibacterial activities.

Authors:  So Rang Kang; Yong Rok Lee
Journal:  Mol Divers       Date:  2015-02-05       Impact factor: 2.943

Review 4.  Factor Xa inhibitors: critical considerations for clinical development and testing.

Authors:  Richard C Becker
Journal:  J Thromb Thrombolysis       Date:  2021-05-15       Impact factor: 2.300

Review 5.  Recent Advances of Pyridinone in Medicinal Chemistry.

Authors:  Shibo Lin; Chun Liu; Xiaotian Zhao; Xiao Han; Xuanhao Li; Yongqin Ye; Zheyu Li
Journal:  Front Chem       Date:  2022-03-23       Impact factor: 5.221

  5 in total

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