Chemical and Pharmaceutical Bulletin
Online ISSN : 1347-5223
Print ISSN : 0009-2363
ISSN-L : 0009-2363
Regular Articles
Structure–Activity Relationships of New N-Acylanthranilic Acid Derivatives as Plasminogen Activator Inhibitor-1 Inhibitors
Nagahisa YamaokaHidehiko KodamaYuko IzuharaToshio MiyataKanji Meguro
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2011 Volume 59 Issue 2 Pages 215-224

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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.

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© 2011 The Pharmaceutical Society of Japan
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