Literature DB >> 18054228

Structure and property based design of factor Xa inhibitors: pyrrolidin-2-ones with biaryl P4 motifs.

Robert J Young1, Alan D Borthwick, David Brown, Cynthia L Burns-Kurtis, Matthew Campbell, Chuen Chan, Marie Charbaut, Chun-wa Chung, Máire A Convery, Henry A Kelly, N Paul King, Savvas Kleanthous, Andrew M Mason, Anthony J Pateman, Angela N Patikis, Ivan L Pinto, Derek R Pollard, Stefan Senger, Gita P Shah, John R Toomey, Nigel S Watson, Helen E Weston.   

Abstract

Structure and property based drug design was exploited in the synthesis of sulfonamidopyrrolidin-2-one-based factor Xa (fXa) inhibitors, incorporating biaryl P4 groups, producing highly potent inhibitors with encouraging oral pharmacokinetic profiles and significant but sub-optimal anticoagulant activities.

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Year:  2007        PMID: 18054228     DOI: 10.1016/j.bmcl.2007.11.023

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


  4 in total

1.  Potent direct inhibitors of factor Xa based on the tetrahydroisoquinoline scaffold.

Authors:  Rami A Al-Horani; Akul Y Mehta; Umesh R Desai
Journal:  Eur J Med Chem       Date:  2012-06-23       Impact factor: 6.514

2.  CSAR 2014: A Benchmark Exercise Using Unpublished Data from Pharma.

Authors:  Heather A Carlson; Richard D Smith; Kelly L Damm-Ganamet; Jeanne A Stuckey; Aqeel Ahmed; Maire A Convery; Donald O Somers; Michael Kranz; Patricia A Elkins; Guanglei Cui; Catherine E Peishoff; Millard H Lambert; James B Dunbar
Journal:  J Chem Inf Model       Date:  2016-05-17       Impact factor: 4.956

3.  Synthesis, Docking, and In Vitro Anticoagulant Activity Assay of Hybrid Derivatives of Pyrrolo[3,2,1-ij]Quinolin-2(1H)-one as New Inhibitors of Factor Xa and Factor XIa.

Authors:  Nadezhda Novichikhina; Ivan Ilin; Anna Tashchilova; Alexey Sulimov; Danil Kutov; Irina Ledenyova; Mikhail Krysin; Khidmet Shikhaliev; Anna Gantseva; Ekaterina Gantseva; Nadezhda Podoplelova; Vladimir Sulimov
Journal:  Molecules       Date:  2020-04-19       Impact factor: 4.411

4.  3-Chloro-3-methyl-2,6-diarylpiperidin-4-ones as Anti-Cancer Agents: Synthesis, Biological Evaluation, Molecular Docking, and In Silico ADMET Prediction.

Authors:  Arulraj Ramalingam; Nurulhuda Mustafa; Wee Joo Chng; Mouna Medimagh; Sivakumar Sambandam; Noureddine Issaoui
Journal:  Biomolecules       Date:  2022-08-08
  4 in total

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