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Design, synthesis and in vitro evaluation of potent, novel, small molecule inhibitors of plasminogen activator inhibitor-1 |
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| Authors: | Folkes Adrian Brown S David Canne Lynne E Chan Jocelyn Engelhardt Erin Epshteyn Sergey Faint Richard Golec Julian Hanel Art Kearney Patrick Leahy James W Mac Morrison Matthews David Prisbylla Michael P Sanderson Jason Simon Reyna J Tesfai Zerom Vicker Nigel Wang Shouming Webb Robert R Charlton Peter |
| Affiliation: | Xenova Limited, 957 Buckingham Avenue, Slough, Berks SL1 4NL, UK. adian_folkes@xenova.co.uk |
| Abstract: | We have synthesized and evaluated a series of tetramic acid-based and hydroxyquinolinone-based inhibitors of plasminogen activator inhibitor-1 (PAI-1). These studies resulted in the identification of several compounds which showed excellent potency against PAI-1. The design, synthesis and SAR of these compounds are described. |
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