Chemical & Pharmaceutical Bulletin 2011-01-01

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

Index: Chem. Pharm. Bull. 59(2) , 215-24, (2011)

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Abstract

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.© 2011 Pharmaceutical Society of Japan