Design of novel aminopyrrolidine factor Xa inhibitors from a screening hit.

Katrin Groebke Zbinden,Lilli Anselm,David W Banner,Jörg Benz,Francesca Blasco,Guillaume Décoret,Jacques Himber,Bernd Kuhn,Narendra Panday,Fabienne Ricklin,Philippe Risch,Daniel Schlatter,Martin Stahl,Stefan Thomi,Robert Unger,Wolfgang Haap

European Journal of Medicinal Chemistry（2009）

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摘要

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.

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关键词

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

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