Structure-Activity Relationships of New N-Acylanthranilic Acid Derivatives as Plasminogen Activator Inhibitor-1 Inhibitors
-
- Yamaoka Nagahisa
- CT Laboratory, Hamari Chemicals, Ltd.
-
- Kodama Hidehiko
- CT Laboratory, Hamari Chemicals, Ltd.
-
- Izuhara Yuko
- Center for Translational and Advanced Research, Tohoku University School of Medicine
-
- Miyata Toshio
- Center for Translational and Advanced Research, Tohoku University School of Medicine
-
- Meguro Kanji
- CT Laboratory, Hamari Chemicals, Ltd.
Search this article
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.
Journal
-
- Chemical and Pharmaceutical Bulletin
-
Chemical and Pharmaceutical Bulletin 59 (2), 215-224, 2011
The Pharmaceutical Society of Japan
- Tweet
Keywords
Details 詳細情報について
-
- CRID
- 1390282679149882240
-
- NII Article ID
- 130000405518
-
- NII Book ID
- AA00602100
-
- ISSN
- 13475223
- 00092363
-
- NDL BIB ID
- 10951877
-
- Text Lang
- en
-
- Data Source
-
- JaLC
- NDL
- Crossref
- CiNii Articles
-
- Abstract License Flag
- Disallowed