title: Structure-activity relationships of new N-acylanthranilic acid derivatives as plasminogen activator inhibitor-1 inhibitors.
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.
authors.affiliation: CT Laboratory, Hamari Chemicals, Ltd., Osaka, Japan. nagahisa-yamaoka@hamari.co.jp
authors.forename: Nagahisa
authors.initials: N
authors.lastname: Yamaoka
authors.forename: Hidehiko
authors.initials: H
authors.lastname: Kodama
authors.forename: Yuko
authors.initials: Y
authors.lastname: Izuhara
authors.forename: Toshio
authors.initials: T
authors.lastname: Miyata
authors.forename: Kanji
authors.initials: K
authors.lastname: Meguro
mesh_terms: D000284:Administration, Oral; D000818:Animals; D006801:Humans; D008297:Male; D017395:Plasminogen Activator Inhibitor 1 / Q000008:administration & dosage* / Q000737:chemistry* / Q000493:pharmacokinetics; D051381:Rats; D017208:Rats, Wistar; D013329:Structure-Activity Relationship; D062367:ortho-Aminobenzoates / Q000008:administration & dosage* / Q000737:chemistry* / Q000493:pharmacokinetics
chemical_list: D017395:Plasminogen Activator Inhibitor 1; D062367:ortho-Aminobenzoates; C031385:anthranilic acid