Synthesis and structure-activity relationships of 7-(2-aminoalkyl)morpholinoquinolones as anti-Helicobacter pylori agents.
A series of the titled compounds was synthesized and tested for anti-Helicobacter pylori activities. We discovered Y-34867 having the most potent activity against Helicobacter pylori among the quinolones tested along with high photostability. Furthermore, Y-34867 showed an excellent therapeutic effect in the experimental Helicobacter pylori infected Mongolian gerbil model.
Sakurai
N
N
Research Laboratory Yoshitomi Pharmaceutical Industries, Ltd., Fukuoka, Japan.
Sano
M
M
Hirayama
F
F
Kuroda
T
T
Uemori
S
S
Moriguchi
A
A
Yamamoto
K
K
Ikeda
Y
Y
Kawakita
T
T
D042462:4-Quinolones; D000818:Animals; D000890:Anti-Infective Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D004355:Drug Stability; D024841:Fluoroquinolones; D005849:Gerbillinae; D016481:Helicobacter Infections / Q000188:drug therapy*; D016480:Helicobacter pylori / Q000187:drug effects*; D007202:Indicators and Reagents; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D009287:Naphthyridines / Q000494:pharmacology; D015242:Ofloxacin / Q000494:pharmacology; D015363:Quinolones / Q000138:chemical synthesis* / Q000737:chemistry* / Q000494:pharmacology / Q000627:therapeutic use; D012996:Solutions; D013329:Structure-Activity Relationship; D014466:Ultraviolet Rays
D042462:4-Quinolones; D000890:Anti-Infective Agents; D024841:Fluoroquinolones; D007202:Indicators and Reagents; D009287:Naphthyridines; D015363:Quinolones; D012996:Solutions; C078061:Y 26611; D015242:Ofloxacin; C055185:tosufloxacin; C061363:sparfloxacin