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Bioorg Med Chem Lett. 2006 Jul 15;16(14):3784-8. Epub 2006 May 11.

Design and synthesis of orally active pyrrolidin-2-one-based factor Xa inhibitors.

Author information

1
GlaxoSmithKline, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, UK. Nigel.S.Watson@gsk.com

Abstract

A series of novel, non-basic 3-(6-chloronaphth-2-ylsulfonyl)aminopyrrolidin-2-one-based factor Xa (fXa) inhibitors, incorporating an alanylamide P4 group, was designed and synthesised. Within this series, the N-2-(morpholin-4-yl)-2-oxoethyl derivative 24 was shown to be a potent, selective fXa inhibitor with good anticoagulant activity. Moreover, 24 possessed highly encouraging rat and dog pharmacokinetic profiles with excellent oral bioavailabilities in both species.

PMID:
16697194
DOI:
10.1016/j.bmcl.2006.04.053
[Indexed for MEDLINE]

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