Novel bis-arylsulfonamides and aryl sulfonimides as inactivators of plasminogen activator inhibitor-1 (PAI-1).

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 Lett

authors

El-Ayache NC,Li SH,Warnock M,Lawrence DA,Emal CD

doi

10.1016/j.bmcl.2009.12.051

subject

Has Abstract

pub_date

2010-02-01 00:00:00

pages

966-70

issue

3

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(09)01774-0

journal_volume

20

pub_type

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