Structure-activity relationships of new 2-acylamino-3-thiophenecarboxylic acid dimers as plasminogen activator inhibitor-1 inhibitors

N Yamaoka, Y Kawano, Y Izuhara, T Miyata…

Index: Yamaoka, Nagahisa; Kawano, Yasuhiko; Izuhara, Yuko; Miyata, Toshio; Meguro, Kanji Chemical and Pharmaceutical Bulletin, 2010 , vol. 58, # 5 p. 615 - 619

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Citation Number: 12

Abstract

Small molecule inhibitors of plasminogen activator inhibitor (PAI)-1 have been reported to date but their clinical effects still remain unknown. The present study was undertaken to investigate the structure–activity relationships (SAR) of newly synthesized 2-acylamino-3- thiophenecarboxylic acid dimers based upon a core structure of TM5001 (1) and TM5007 (2) that we have previously identified as orally effective PAI-1 inhibitors. In general, ...