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

Research output: Contribution to journalArticlepeer-review

7 Citations (Scopus)

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.

Original languageEnglish
Pages (from-to)215-224
Number of pages10
JournalChemical and Pharmaceutical Bulletin
Volume59
Issue number2
DOIs
Publication statusPublished - 2011 Feb

Keywords

  • Inhibitor
  • N-acylanthranilic acid derivative
  • Plasminogen activator inhibitor-1
  • Structure-activity relationship
  • TM5275

ASJC Scopus subject areas

  • Chemistry(all)
  • Drug Discovery

Fingerprint

Dive into the research topics of 'Structure-activity relationships of new N-acylanthranilic acid derivatives as plasminogen activator inhibitor-1 inhibitors'. Together they form a unique fingerprint.

Cite this