Discovery of a novel benzyloxyisoquinoline derivative with potent anti- Helicobacter pylori activity

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 activit...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 1998-07, Vol.8 (14), p.1897-1902
Main Authors: Yoshida, Yoshiki, Barrett, David, Azami, Hidenori, Morinaga, Chizu, Matsumoto, Yoshimi, Takasugi, Hisashi
Format: Article
Language:English
Subjects:
Acetamides - chemical synthesis
Acetamides - chemistry
Acetamides - pharmacology
Animals
Anti-Bacterial Agents - chemical synthesis
Anti-Bacterial Agents - chemistry
Anti-Bacterial Agents - pharmacology
Antibacterial agents
Antibacterials
Antibiotics. Antiinfectious agents. Antiparasitic agents
Antimicrobial compds
Bacteria
Biological and medical sciences
Digestive system
Gastrointestinal activity
Helicobacter pylori - drug effects
Isoquinolines - chemical synthesis
Isoquinolines - chemistry
Isoquinolines - pharmacology
Magnetic Resonance Spectroscopy
Medical sciences
Mice
Microbial Sensitivity Tests
Pharmacology. Drug treatments
Structure-Activity Relationship
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Summary: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. The synthesis and in vitro optimization of the anti- H.pylori activity of a series of novel benzyloxyisoquinoline derivatives are described. FR180102, having a 3-acetamido-2,6-dichlorobenzyl moiety, was found to have extremely potent activity.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(98)00335-7