4.7 Article

Design of novel aminopyrrolidine factor Xa inhibitors from a screening hit

Journal

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 44, Issue 7, Pages 2787-2795

Publisher

ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2008.12.025

Keywords

Anticoagulant; Oral bioavailability; Factor Xa inhibitor; Biased screen; Computer-aided design; X-ray analysis; Clotting assay

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Starting from a hit identified by focused screening, 3-aminopyrrolidine factor Xa inhibitors were designed. The binding mode as determined by X-ray structural analysis as well as the pharmacokinetic behaviour of selected compounds is discussed. (C) 2009 Elsevier Masson SAS. All rights reserved.

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