Structure–Activity Relationships of New 2-Acylamino-3-thiophenecarboxylic Acid Dimers as Plasminogen Activator Inhibitor-1 Inhibitors
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概要
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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, compounds possessing bulky or/and hydrophobic substituents (e.g. phenyl, isobutyl group) on the both thiophene rings showed potent PAI-1 inhibitory activities irrespective of the positions of the substitution. The mono-carboxyl derivative (10) exhibited PAI-1 inhibition comparable to the corresponding dicarboxyl compound (9f).
著者
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Yamaoka Nagahisa
CT Laboratory, Hamari Chemicals, Ltd.
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Miyata Toshio
Center for Translational and Advanced Research, Tohoku University School of Medicine
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Meguro Kanji
CT Laboratory, Hamari Chemicals, Ltd.
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Miyata Toshio
Center For Translational And Advanced Research Tohoku University Graduate School Of Medicine Tohoku
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Kawano Yasuhiko
CT Laboratory, Hamari Chemicals, Ltd.
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Izuhara Yuko
Institute of Medical Sciences and Division of Nephrology, Hypertension and Metabolism, Department of
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Miyata Toshio
Center For Translational And Advanced Research Tohoku University Graduate School Of Medicine
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Izuhara Yuko
Institute of Medical Sciences and Division of Nephrology, Hypertension and Metabolism, Department of Internal Medicine, Tokai University School of Medicine
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