title: Synthesis and structure-activity relationships of 7-(2-aminoalkyl)morpholinoquinolones as anti-Helicobacter pylori agents.
abstract: 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.
authors.affiliation: Research Laboratory Yoshitomi Pharmaceutical Industries, Ltd., Fukuoka, Japan.
authors.forename: N
authors.initials: N
authors.lastname: Sakurai
authors.forename: M
authors.initials: M
authors.lastname: Sano
authors.forename: F
authors.initials: F
authors.lastname: Hirayama
authors.forename: T
authors.initials: T
authors.lastname: Kuroda
authors.forename: S
authors.initials: S
authors.lastname: Uemori
authors.forename: A
authors.initials: A
authors.lastname: Moriguchi
authors.forename: K
authors.initials: K
authors.lastname: Yamamoto
authors.forename: Y
authors.initials: Y
authors.lastname: Ikeda
authors.forename: T
authors.initials: T
authors.lastname: Kawakita
mesh_terms: 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
chemical_list: 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