Literature DB >> 12668020

Oxyguanidines: application to non-peptidic phenyl-based thrombin inhibitors.

Bruce Tomczuk1, Tianbao Lu, Richard M Soll, Cynthia Fedde, Aihua Wang, Larry Murphy, Carl Crysler, Malini Dasgupta, Stephen Eisennagel, John Spurlino, Roger Bone.   

Abstract

Although thrombin has been extensively researched with many examples of potent and selective inhibitors, the key characteristics of oral bioavailability and long half-life have been elusive. We report here a novel series non-peptidic phenyl-based, highly potent, highly selective and orally bioavailable thrombin inhibitors using oxyguanidines as guanidine-mimetics.

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Year:  2003        PMID: 12668020     DOI: 10.1016/s0960-894x(03)00125-2

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


  4 in total

1.  Synthesis and Evaluation of Oxyguanidine Analogues of the Cysteine Protease Inhibitor WRR-483 against Cruzain.

Authors:  Brian D Jones; Anna Tochowicz; Yinyan Tang; Michael D Cameron; Laura-Isobel McCall; Ken Hirata; Jair L Siqueira-Neto; Sharon L Reed; James H McKerrow; William R Roush
Journal:  ACS Med Chem Lett       Date:  2015-12-15       Impact factor: 4.345

2.  New synthetic thrombin inhibitors: molecular design and experimental verification.

Authors:  Elena I Sinauridze; Alexey N Romanov; Irina V Gribkova; Olga A Kondakova; Stepan S Surov; Aleksander S Gorbatenko; Andrey A Butylin; Mikhail Yu Monakov; Alexey A Bogolyubov; Yuryi V Kuznetsov; Vladimir B Sulimov; Fazoyl I Ataullakhanov
Journal:  PLoS One       Date:  2011-05-16       Impact factor: 3.240

3.  The Basicity Makes the Difference: Improved Canavanine-Derived Inhibitors of the Proprotein Convertase Furin.

Authors:  Thuy Van Lam van; Miriam Ruth Heindl; Christine Schlutt; Eva Böttcher-Friebertshäuser; Ralf Bartenschlager; Gerhard Klebe; Hans Brandstetter; Sven O Dahms; Torsten Steinmetzer
Journal:  ACS Med Chem Lett       Date:  2021-02-09       Impact factor: 4.345

4.  Study of the Differential Activity of Thrombin Inhibitors Using Docking, QSAR, Molecular Dynamics, and MM-GBSA.

Authors:  Karel Mena-Ulecia; William Tiznado; Julio Caballero
Journal:  PLoS One       Date:  2015-11-24       Impact factor: 3.240

  4 in total

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