1103929-96-9Relevant academic research and scientific papers
Structure-activity relationships of new N-acylanthranilic acid derivatives as plasminogen activator inhibitor-1 inhibitors
Yamaoka, Nagahisa,Kodama, Hidehiko,Izuhara, Yuko,Miyata, Toshio,Meguro, Kanji
, p. 215 - 224 (2011/04/16)
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.
PLASMINOGEN ACTIVATOR INHIBITOR-1 INHIBITOR
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Page/Page column 51, (2009/05/28)
The present invention relates to an inhibitor of plasminogen activator inhibitor-1. The present invention further relates to a pharmaceutical composition that has an inhibitory action on PAI-1 activity and is useful in the prevention and treatment of various diseases whose onset is associated with PAI-1 activity. Furthermore, the present invention relates to a novel compound having PAI-1 inhibitory activity represented by the following general formula (I), and a salt thereof. Each symbol is defined as those in the specification.
