Synthesis and antibacterial activity of novel 7-(3-substituted-3 or 4-trifluoromethyl-1-pyrrolidinyl)-8-methoxyfluoroquinolones.
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.
Fukui
H
H
Central Research Institute, Kaken Pharmaceutical Co., Ltd., Kyoto, Japan.
Shibata
T
T
Naito
T
T
Nakano
J
J
Maejima
T
T
Senda
H
H
Iwatani
W
W
Tatsumi
Y
Y
Suda
M
M
Arika
T
T
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*
D000890:Anti-Infective Agents; D024841:Fluoroquinolones; D011759:Pyrrolidines; C116812:S 34109