title: Synthesis and antibacterial activity of novel 7-(3-substituted-3 or 4-trifluoromethyl-1-pyrrolidinyl)-8-methoxyfluoroquinolones.
abstract: The titled compounds were synthesized and evaluated for in vitro antibacterial activity. The (3R, 4S)-3-aminomethyl-4-trifluoromethyl derivative (S-34109) was confirmed to be optimal because of its superior activity against quinolone and methicillin-resistant Staphylococcus aureus and low side effect potential.
authors.affiliation: Central Research Institute, Kaken Pharmaceutical Co., Ltd., Kyoto, Japan.
authors.forename: H
authors.initials: H
authors.lastname: Fukui
authors.forename: T
authors.initials: T
authors.lastname: Shibata
authors.forename: T
authors.initials: T
authors.lastname: Naito
authors.forename: J
authors.initials: J
authors.lastname: Nakano
authors.forename: T
authors.initials: T
authors.lastname: Maejima
authors.forename: H
authors.initials: H
authors.lastname: Senda
authors.forename: W
authors.initials: W
authors.lastname: Iwatani
authors.forename: Y
authors.initials: Y
authors.lastname: Tatsumi
authors.forename: M
authors.initials: M
authors.lastname: Suda
authors.forename: T
authors.initials: T
authors.lastname: Arika
mesh_terms: D000890:Anti-Infective Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D018432:Drug Resistance, Multiple; D024841:Fluoroquinolones; D006090:Gram-Negative Bacteria / Q000187:drug effects; D006094:Gram-Positive Bacteria / Q000187:drug effects; D016106:Methicillin Resistance; D008826:Microbial Sensitivity Tests; D011759:Pyrrolidines / Q000138:chemical synthesis* / Q000494:pharmacology; D013211:Staphylococcus aureus / Q000187:drug effects*
chemical_list: D000890:Anti-Infective Agents; D024841:Fluoroquinolones; D011759:Pyrrolidines; C116812:S 34109