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 (3 R,4 S)-3-aminomethyl-4-trifluoromethyl derivative (S-34109) was confirmed to be optimal because of its superior activity against quinolone and methicillin-resistant Staphyrococcus aureus and low side effe...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 1998-10, Vol.8 (20), p.2833-2838
Hauptverfasser:	Fukui, Hideto, Shibata, Tetsuo, Naito, Takanobu, Nakano, Jun, Maejima, Tetsuro, Senda, Hisato, Iwatani, Wakao, Tatsumi, Yoshiyuki, Suda, Masahiro, Arika, Ta-i
Format:	Artikel
Sprache:	eng
Schlagworte:	Anti-Infective Agents - chemical synthesis Anti-Infective Agents - pharmacology Antibacterial agents antibacterials Antibiotics. Antiinfectious agents. Antiparasitic agents bacteria Biological and medical sciences chemotherapy Drug Resistance, Multiple Fluoroquinolones Gram-Negative Bacteria - drug effects Gram-Positive Bacteria - drug effects Medical sciences Methicillin Resistance Microbial Sensitivity Tests Pharmacology. Drug treatments Pyrrolidines - chemical synthesis Pyrrolidines - pharmacology Staphylococcus aureus - drug effects
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Zusammenfassung:	The titled compounds were synthesized and evaluated for in vitro antibacterial activity. The (3 R,4 S)-3-aminomethyl-4-trifluoromethyl derivative (S-34109) was confirmed to be optimal because of its superior activity against quinolone and methicillin-resistant Staphyrococcus aureus and low side effect potential. The titled compounds were synthesized and evaluated for in vitro antibacterial activity. The (3 R,4 S)-3-aminomethyl-4-trifluoromethyl derivative (S-34109) was confirmed to be optimal because of its superior activity against quinolone and methicillin-resistant Staphyrococcus aureus and low side-effect potential.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/S0960-894X(98)00514-9