Chemical and Pharmaceutical Bulletin
Online ISSN : 1347-5223
Print ISSN : 0009-2363
ISSN-L : 0009-2363
Regular Articles
Synthesis and Evaluation of 1-Arylsulfonyl-3-piperazinone Derivatives as Factor Xa Inhibitor
Hidemitsu NISHIDA, Yutaka MiYAZAKI, Yoshihiro KITAMURA, Masayuki OHASHI, Tomokazu MATSUSUE, Atsushi OKAMOTO, Yoshitaka HOSAKA, Shuhei OHNISHI, Hidenori MOCHIZUKI
Author information
Keywords: factor Xa inhibitor, 4-(piperidino)pyridine, structure-activity relationship, M55113
JOURNAL FREE ACCESS

2001 Volume 49 Issue 10 Pages 1237-1244

Details
Download PDF (99K)
Download citation RIS

(compatible with EndNote, Reference Manager, ProCite, RefWorks)

BIB TEX

(compatible with BibDesk, LaTeX)

Text
How to download citation
Contact us
Abstract

Intravascular clot formation is an important factor in a number of cardiovascular diseases. Therefore, the prevention of blood coagulation has become a major target for new therapeutic agents. One attractive approach is the inhibition of factor Xa (FXa), which is a key enzyme in coagulation cascade responsible for the generation of thrombin by limited proteolysis of its zymogen, prothrombin. We have investigated 1-arylsulfonyl-3-piperazinone derivatives, containing a 4-(piperidino)pyridine group in place of guanidino and/or amidino groups, and discovered compound M55113 (30a: 4-[(6-Chloro-2-naphthalenyl)sulfonyl]-1-[[1-(4-pyridinyl)-4-piperidinyl]-methyl]piperazinone), as a potent inhibitor of FXa (IC50=0.06 μM) with high selectivity for FXa over trypsin and thrombin.

Content from these authors
© 2001 The Pharmaceutical Society of Japan
Next article
Favorites & Alerts

Recently viewed articles
Share this page
feedback
 Top