Title of article
Synthesis and evaluation of 1,4-diphenylbutadiene derivatives as inhibitors of plasminogen activator inhibitor-1 (PAI-1) production Original Research Article
Author/Authors
Hiroshi Miyazaki، نويسنده , , Hiroshi Sai، نويسنده , , Hiroshi Ohmizu، نويسنده , , Jun Murakami، نويسنده , , Akio Ohtani، نويسنده , , Tsuyoshi Ogiku، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2010
Pages
12
From page
1968
To page
1979
Abstract
Butadiene-imide 1 (T-686) derivatives were synthesized and evaluated for their inhibitory activity against PAI-1 production and their ADMET (DMPK and toxicology) profiles. Among these derivatives, compound 15k (T-2639) showed good antithrombotic activity in two rat thrombosis models without affecting bleeding time, indicating reduction of haemorrhagic risk. We also describe in this report a practical synthesis of 15k suitable for scale-up using Z,E-selective Stobbe condensation.
Keywords
Plasminogen activator inhibitor-1 , T-2639 , Inhibitor of PAI-1 production
Journal title
Bioorganic and Medicinal Chemistry
Serial Year
2010
Journal title
Bioorganic and Medicinal Chemistry
Record number
1307198
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