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

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

MED - United Centers for Advanced Research and Translational Medicine (ART)

Research output: Contribution to journal › Article › peer-review

8 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 language	English
Pages (from-to)	215-224
Number of pages	10
Journal	Chemical and Pharmaceutical Bulletin
Volume	59
Issue number	2
DOIs	https://doi.org/10.1248/cpb.59.215
Publication status	Published - 2011 Feb

Keywords

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

ASJC Scopus subject areas

Chemistry(all)
Drug Discovery

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10.1248/cpb.59.215

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AU - Izuhara, Yuko

AU - Miyata, Toshio

AU - Meguro, Kanji

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AB - 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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KW - Plasminogen activator inhibitor-1

KW - Structure-activity relationship

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Structure-activity relationships of new N-acylanthranilic acid derivatives as plasminogen activator inhibitor-1 inhibitors

Abstract

Keywords

ASJC Scopus subject areas

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