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Bioorg Med Chem Lett. 2010 Jan 15;20(2):618-22. doi: 10.1016/j.bmcl.2009.11.077. Epub 2009 Nov 20.

Structure and property based design of factor Xa inhibitors: pyrrolidin-2-ones with monoaryl P4 motifs.

Author information

1
GlaxoSmithKline, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, United Kingdom.

Abstract

Structure and property based drug design was exploited in the synthesis of sulfonamidopyrrolidin-2-one-based factor Xa inhibitors, incorporating neutral and basic monoaryl P4 groups, ultimately producing potent inhibitors with effective levels of anticoagulant activity and extended oral pharmacokinetic profiles. However, time dependant inhibition of Cytochrome P450 3A4 was a particular issue with this series.

PMID:
20006499
DOI:
10.1016/j.bmcl.2009.11.077
[Indexed for MEDLINE]

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