206883-01-4Relevant articles and documents
Studies on anti-Helicobacter pylori agents. Part 1: Benzyloxyisoquinoline derivatives
Yoshida, Yoshiki,Barrett, David,Azami, Hidenori,Morinaga, Chizu,Matsumoto, Satoru,Matsumoto, Yoshimi,Takasugi, Hisashi
, p. 2647 - 2666 (2011/05/18)
The synthesis and optimization of the anti-Helicobacter pylori activity of a novel series of benzyloxyisoquinoline derivatives that was discovered by a random screening process, are described. In the in vitro assay, compound 10c containing a 3-acetamido-2,6-dichlorobenzyl substituent was found to have extremely potent activity against H. pylori and no activity against other common bacteria. The anti-H. pylori activity of 10c was superior to that of amoxicillin (AMPC) (1) and clarithromycin (CAM) (2). However, 10c did not show in vivo efficacy in a mouse infection model; a feature attributed to the lack of strong bactericidal activity at short contact times. (C) 1999 Elsevier Science Ltd.
Discovery of a novel benzyloxyisoquinoline derivative with potent anti- Helicobacter pylori activity
Yoshida, Yoshiki,Barrett, David,Azami, Hidenori,Morinaga, Chizu,Matsumoto, Yoshimi,Takasugi, Hisashi
, p. 1897 - 1902 (2007/10/03)
The synthesis and in vitro optimization of the anti-Helicobacter pylori activity of a novel series of benzyloxyisoquinoline derivatives discovered by a random screening process, are described. FR180102 (7f), having a 3- acetamido-2,6-dichlorobenzyl moiety, was found to have extremely potent activity against H. pylori and no effect against a series of common Gram- positive and Gram-negative bacteria.