Journal
CHEMICAL & PHARMACEUTICAL BULLETIN
Volume 59, Issue 2, Pages 215-224Publisher
PHARMACEUTICAL SOC JAPAN
DOI: 10.1248/cpb.59.215
Keywords
plasminogen activator inhibitor-1; inhibitor; N-acylanthranilic acid derivative; structure activity relationship; TM5275
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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-piper-azinyl 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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