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

Nagahisa Yamaoka; Hidehiko Kodama; Yuko Izuhara; Toshio Miyata; Kanji Meguro

doi:10.1248/cpb.59.215

Regular Articles

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

Nagahisa Yamaoka, Hidehiko Kodama, Yuko Izuhara, Toshio Miyata, Kanji Meguro

著者情報

キーワード: plasminogen activator inhibitor-1, inhibitor, N-acylanthranilic acid derivative, structure–activity relationship, TM5275

ジャーナルフリー

2011 年 59 巻 2 号 p. 215-224

DOI https://doi.org/10.1248/cpb.59.215

詳細

抄録

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.

責任著者(Corresponding author)

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