Literature DB >> 28105277

Design and Synthesis of Novel Meta-Linked Phenylglycine Macrocyclic FVIIa Inhibitors.

Jeremy M Richter1, Daniel L Cheney1, J Alex Bates1, Anzhi Wei1, Joseph M Luettgen1, Alan R Rendina1, Timothy M Harper1, Rangaraj Narayanan1, Pancras C Wong1, Dietmar Seiffert1, Ruth R Wexler1, E Scott Priestley1.   

Abstract

Two novel series of meta-linked phenylglycine-based macrocyclic FVIIa inhibitors have been designed to improve the rodent metabolic stability and PK observed with the precursor para-linked phenylglycine macrocycles. Through iterative structure-based design and optimization, the TF/FVIIa Ki was improved to subnanomolar levels with good clotting activity, metabolic stability, and permeability.

Entities:  

Keywords:  FVIIa; anticoagulant; antithrombotic; factor VIIa; macrocycle; thrombosis

Year:  2016        PMID： 28105277      PMCID： PMC5238462          DOI： 10.1021/acsmedchemlett.6b00375

Source DB:  PubMed          Journal:  ACS Med Chem Lett        ISSN： 1948-5875            Impact factor:   4.345


  27 in total

1.  New software for searching the Cambridge Structural Database and visualizing crystal structures.

Authors:  Ian J Bruno; Jason C Cole; Paul R Edgington; Magnus Kessler; Clare F Macrae; Patrick McCabe; Jonathan Pearson; Robin Taylor
Journal:  Acta Crystallogr B       Date:  2002-05-29

2.  Recombinant nematode anticoagulant protein c2, an inhibitor of the tissue factor/factor VIIa complex, in patients undergoing elective coronary angioplasty.

Authors:  Arno H M Moons; Ron J G Peters; Nick R Bijsterveld; Jan J Piek; Martin H Prins; George P Vlasuk; William E Rote; Harry R Büller
Journal:  J Am Coll Cardiol       Date:  2003-06-18       Impact factor: 24.094

3.  Efforts toward oral bioavailability in factor VIIa inhibitors.

Authors:  Dange Vijaykumar; Roopa Rai; Michael Shaghafi; Tony Ton; Steve Torkelson; Ellen M Leahy; Jennifer R Riggs; Huiyong Hu; Paul A Sprengeler; William D Shrader; Colin O'Bryan; Ronnell Cabuslay; Ellen Sanford; Erik Gjerstadt; Liang Liu; Juthamas Sukbuntherng; Wendy B Young
Journal:  Bioorg Med Chem Lett       Date:  2006-05-02       Impact factor: 2.823

4.  Dose-dependent antithrombotic activity of an orally active tissue factor/factor VIIa inhibitor without concomitant enhancement of bleeding propensity.

Authors:  Katrin Groebke Zbinden; David W Banner; Kurt Hilpert; Jacques Himber; Thierry Lavé; Markus A Riederer; Martin Stahl; Thomas B Tschopp; Ulrike Obst-Sander
Journal:  Bioorg Med Chem       Date:  2006-04-18       Impact factor: 3.641

5.  The antithrombotic and anti-inflammatory effects of BCX-3607, a small molecule tissue factor/factor VIIa inhibitor.

Authors:  C Shane Arnold; Cynthia Parker; Ramanda Upshaw; Hans Prydz; Pooran Chand; Pravin Kotian; Shanta Bantia; Y Sudhakar Babu
Journal:  Thromb Res       Date:  2006       Impact factor: 3.944

6.  Factor VIIa inhibitors: chemical optimization, preclinical pharmacokinetics, pharmacodynamics, and efficacy in an arterial baboon thrombosis model.

Authors:  Wendy B Young; Joyce Mordenti; Steven Torkelson; William D Shrader; Aleksandr Kolesnikov; Roopa Rai; Liang Liu; Huiyong Hu; Ellen M Leahy; Michael J Green; Paul A Sprengeler; Bradley A Katz; Christine Yu; James W Janc; Kyle C Elrod; Ulla M Marzec; Stephen R Hanson
Journal:  Bioorg Med Chem Lett       Date:  2006-01-18       Impact factor: 2.823

7.  Assessment of bleeding propensity in non-human primates by combination of selective tissue factor/VIIa inhibition and aspirin compared to warfarin and aspirin treatment.

Authors:  Anita K Salyers; James A Szalony; Osman D Suleymanov; John J Parlow; Rhonda S Wood; Michael S South; Nancy S Nicholson
Journal:  Pharmacology       Date:  2004-02       Impact factor: 2.547

8.  Discovery of a Highly Potent, Selective, and Orally Bioavailable Macrocyclic Inhibitor of Blood Coagulation Factor VIIa-Tissue Factor Complex.

Authors:  Xiaojun Zhang; Peter W Glunz; James A Johnson; Wen Jiang; Swanee Jacutin-Porte; Vladimir Ladziata; Yan Zou; Monique S Phillips; Nicholas R Wurtz; Brandon Parkhurst; Alan R Rendina; Timothy M Harper; Daniel L Cheney; Joseph M Luettgen; Pancras C Wong; Dietmar Seiffert; Ruth R Wexler; E Scott Priestley
Journal:  J Med Chem       Date:  2016-08-02       Impact factor: 7.446

9.  Administration of a small molecule tissue factor/factor VIIa inhibitor in a non-human primate thrombosis model of venous thrombosis: effects on thrombus formation and bleeding time.

Authors:  James A Szalony; Osman D Suleymanov; Anita K Salyers; Susan G Panzer-Knodle; Jason D Blom; Rhonda M LaChance; Brenda L Case; John J Parlow; Michael S South; Rhonda S Wood; Nancy S Nicholson
Journal:  Thromb Res       Date:  2003       Impact factor: 3.944

Review 10.  Inhibitors of Factor VIIa/tissue factor.

Authors:  Rebecca A Shirk; George P Vlasuk
Journal:  Arterioscler Thromb Vasc Biol       Date:  2007-06-28       Impact factor: 8.311
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  1 in total

1.  Reactivity and Synthetic Applications of Multicomponent Petasis Reactions.

Authors:  Peng Wu; Michael Givskov; Thomas E Nielsen
Journal:  Chem Rev       Date:  2019-08-27       Impact factor: 60.622
  1 in total

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