Abstract:
:Inactivators of plasminogen activator inhibitor-1 (PAI-1) have been identified as possible treatments for a range of conditions, including atherosclerosis, venous thrombosis, and obesity. We describe the synthesis and inhibitory activity of a novel series of compounds based on bis-arylsulfonamide and aryl sulfonimide motifs that show potent and specific activity towards PAI-1. Inhibitors containing short linking units between the sulfonyl moieties and a 3,4-dihydroxy aryl substitution pattern showed the most potent inhibitory activity, and retained high specificity for PAI-1 over the structurally-related serpin anti-thrombin III (ATIII).
journal_name
Bioorg Med Chem Lettjournal_title
Bioorganic & medicinal chemistry lettersauthors
El-Ayache NC,Li SH,Warnock M,Lawrence DA,Emal CDdoi
10.1016/j.bmcl.2009.12.051subject
Has Abstractpub_date
2010-02-01 00:00:00pages
966-70issue
3eissn
0960-894Xissn
1464-3405pii
S0960-894X(09)01774-0journal_volume
20pub_type
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