Chemical and Pharmaceutical Bulletin
Online ISSN : 1347-5223
Print ISSN : 0009-2363
ISSN-L : 0009-2363
Regular Articles
Indoline Derivatives I: Synthesis and Factor Xa (FXa) Inhibitory Activities
Tetsuji Noguchi, Naoki Tanaka, Toyoki Nishimata, Riki Goto, Miho Hayakawa, Atsuhiro Sugidachi, Taketoshi Ogawa, Fumitoshi Asai, Yumi Matsui, Koichi Fujimoto
Author information
Keywords: Facter Xa (FXa) inhibitory activity, indoline derivative, anticoagulant
JOURNAL FREE ACCESS

2006 Volume 54 Issue 2 Pages 163-174

Details
Download PDF (864K)
Download citation RIS

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

BIB TEX

(compatible with BibDesk, LaTeX)

Text
How to download citation
Contact us
Abstract

A series of bisamidine derivatives each having a ring structure in the center of the molecule was synthesized and their Factor Xa (FXa) inhibitory activities were evaluated. Among them, some indoline derivatives showed potent inhibitory activities in vitro. In particular, (R)-18a having an (R)-configuration at the 2-position of the indoline ring exhibited the most potent FXa inhibitory activity in vitro, more potent than DX-9065a. Furthermore, (R)-18a exhibited more potent anticoagulant activity than DX-9065a. We also succeeded in obtaining an X-ray crystal structure of FXa bound with (R)-18a.

Content from these authors
© 2006 The Pharmaceutical Society of Japan
Previous article Next article
Favorites & Alerts

Recently viewed articles
Share this page
feedback
 Top