Structure–Activity Relationships of New N-Acylanthranilic Acid Derivatives as Plasminogen Activator Inhibitor-1 Inhibitors

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概要

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• Novel anthranilic acid derivatives having substituted N-acyl side chains were designed and synthesized for evaluation as plasminogen activator inhibitor-1 (PAI-1) inhibitors. Compounds with a 4-diphenylmethyl-1-piperazinyl moiety on the acyl side chains in general exhibited potent in vitro PAI-1 inhibitory activity and good pharmacokinetic profiles after oral administration in rats. Compound 16f (TM5275) was identified as a promising candidate for further pharmacological evaluation.

著者

• Yamaoka Nagahisa

  CT Laboratory, Hamari Chemicals, Ltd.

• Kodama Hidehiko

  CT Laboratory, Hamari Chemicals, Ltd.

• Izuhara Yuko

  Center for Translational and Advanced Research, Tohoku University School of Medicine

• Miyata Toshio

  Center for Translational and Advanced Research, Tohoku University School of Medicine

• Meguro Kanji

  CT Laboratory, Hamari Chemicals, Ltd.

• Miyata Toshio

  Center For Translational And Advanced Research Tohoku University Graduate School Of Medicine Tohoku

• Miyata Toshio

  Center For Translational And Advanced Research Tohoku University Graduate School Of Medicine

関連論文

• Structure-activity relationships of new N-acylanthranilic acid derivatives as plasminogen activator inhibitor-1 inhibitors
• Structure–Activity Relationships of New N-Acylanthranilic Acid Derivatives as Plasminogen Activator Inhibitor-1 Inhibitors
• Structure–Activity Relationships of New 2-Acylamino-3-thiophenecarboxylic Acid Dimers as Plasminogen Activator Inhibitor-1 Inhibitors
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