Literature DB >> 15125936

Novel factor Xa inhibitors based on a benzoic acid scaffold and incorporating a neutral P1 ligand.

Marc Nazaré1, Hans Matter, Otmar Klingler, Fahad Al-Obeidi, Herman Schreuder, Gerhard Zoller, Jörg Czech, Martin Lorenz, Angela Dudda, Anusch Peyman, Hans Peter Nestler, Matthias Urmann, Armin Bauer, Volker Laux, Volkmar Wehner, David W Will.   

Abstract

A series of novel, highly potent, achiral factor Xa inhibitors based on a benzoic acid scaffold and containing a chlorophenethyl moiety directed towards the protease S1 pocket is described. A number of structural features, such as the requirements of the P1, P4 and ester-binding pocket ligands were explored with respect to inhibition of factor Xa. Compound 46 was found to be the most potent compound in a series of antithrombotic secondary assays.

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Year:  2004        PMID: 15125936     DOI: 10.1016/j.bmcl.2004.03.059

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


  1 in total

1.  Computational model for predicting chemical substituent effects on passive drug permeability across parallel artificial membranes.

Authors:  Chayan Acharya; Paul R Seo; James E Polli; Alexander D Mackerell
Journal:  Mol Pharm       Date:  2008-08-19       Impact factor: 4.939

  1 in total

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