Literature DB >> 21035339

Design and synthesis of macrocyclic indoles targeting blood coagulation cascade Factor XIa.

Stephen Hanessian1, Andreas Larsson, Tomas Fex, Wolfgang Knecht, Niklas Blomberg.   

Abstract

The synthesis of a series of novel macrocyclic compounds designed to target blood coagulation Factor XIa is described. The compounds were evaluated for their inhibition of a small set of serine proteases. Several compounds displayed modest activity and good selectivity for Factor XIa. Within the series, a promising lead structure for developing novel macrocyclic inhibitors of thrombin was identified.
Copyright © 2010 Elsevier Ltd. All rights reserved.

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Year:  2010        PMID： 21035339     DOI： 10.1016/j.bmcl.2010.09.141

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


  9 in total

1.  High-resolution crystal structures of factor XIa coagulation factor in complex with nonbasic high-affinity synthetic inhibitors.

Authors:  Xavier Fradera; Bert Kazemier; Emma Carswell; Andrew Cooke; Arthur Oubrie; William Hamilton; Maureen Dempster; Stephan Krapp; Susanna Nagel; Anja Jestel
Journal:  Acta Crystallogr Sect F Struct Biol Cryst Commun       Date:  2012-03-27

Review 2.  Recent advances in the discovery and development of factor XI/XIa inhibitors.

Authors:  Rami A Al-Horani; Daniel K Afosah
Journal:  Med Res Rev       Date:  2018-05-04       Impact factor: 12.944

3.  Discovery of allosteric modulators of factor XIa by targeting hydrophobic domains adjacent to its heparin-binding site.

Authors:  Rajesh Karuturi; Rami A Al-Horani; Shrenik C Mehta; David Gailani; Umesh R Desai
Journal:  J Med Chem       Date:  2013-03-18       Impact factor: 7.446

4.  Sulfated pentagalloylglucoside is a potent, allosteric, and selective inhibitor of factor XIa.

Authors:  Rami A Al-Horani; Pooja Ponnusamy; Akul Y Mehta; David Gailani; Umesh R Desai
Journal:  J Med Chem       Date:  2013-01-28       Impact factor: 7.446

Review 5.  Factor XIa inhibitors: A review of the patent literature.

Authors:  Rami A Al-Horani; Umesh R Desai
Journal:  Expert Opin Ther Pat       Date:  2016       Impact factor: 6.674

6.  Enantioselective Radical Construction of 5-Membered Cyclic Sulfonamides by Metalloradical C-H Amination.

Authors:  Yang Hu; Kai Lang; Chaoqun Li; Joseph B Gill; Isaac Kim; Hongjian Lu; Kimberly B Fields; McKenzie Marshall; Qigan Cheng; Xin Cui; Lukasz Wojtas; X Peter Zhang
Journal:  J Am Chem Soc       Date:  2019-11-01       Impact factor: 15.419

7.  Creating novel activated factor XI inhibitors through fragment based lead generation and structure aided drug design.

Authors:  Ola Fjellström; Sibel Akkaya; Hans-Georg Beisel; Per-Olof Eriksson; Karl Erixon; David Gustafsson; Ulrik Jurva; Daiwu Kang; David Karis; Wolfgang Knecht; Viveca Nerme; Ingemar Nilsson; Thomas Olsson; Alma Redzic; Robert Roth; Jenny Sandmark; Anna Tigerström; Linda Öster
Journal:  PLoS One       Date:  2015-01-28       Impact factor: 3.240

8.  Designing allosteric inhibitors of factor XIa. Lessons from the interactions of sulfated pentagalloylglucopyranosides.

Authors:  Rami A Al-Horani; Umesh R Desai
Journal:  J Med Chem       Date:  2014-05-29       Impact factor: 7.446

9.  Modular, One-Pot, Sequential Aziridine Ring Opening-S(N)Ar Strategy to 7-, 10-, and 11-Membered Benzo-Fused Sultams.

Authors:  Joanna K Loh; Naeem Asad; Thiwanka B Samarakoon; Paul R Hanson
Journal:  J Org Chem       Date:  2015-10-08       Impact factor: 4.354
  9 in total

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