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Synthesis and antibacterial activity of the 4-quinolone-3-carboxylic acid derivatives having a trifluoromethyl group as a novel N-1 substituent.

Journal of medicinal chemistry (2005-04-29)
Yoshikazu Asahina, Ichiro Araya, Kazuhiko Iwase, Fujio Iinuma, Masaki Hosaka, Takayoshi Ishizaki
ABSTRACT

Novel 1-trifluoromethyl-4-quinolone derivatives (8a,b) were synthesized, and the antibacterial activity of each was evaluated. An oxidative desulfurization-fluorination reaction was employed to introduce a trifluoromethyl group at the N-1 position as a key step. Among the derivatives, 8a was found to exhibit antibacterial activity comparable to that of norfloxacin (1) against Staphylococcus aureus Smith, Streptococcus pneumoniae IID1210, and Escherichia coli NIHJ JC-2.

MATERIALS
Product Number
Brand
Product Description

Supelco
Norfloxacin, analytical standard, ≥98% (TLC)
Supelco
Norfloxacin, VETRANAL®, analytical standard