Protonation equilibrium and lipophilicity of olamufloxacin (HSR-903), a newly synthesized fluoroquinolone antibacterial

Quinolone Antibiotics: The Development of Moxifloxacin

“…As with clinafloxacin, tosufloxacin 12, which was also withdrawn from the market, has a 3-amino-1-pyrrolidinyl radical in the 7-position. This useful substituent was modified by attaching additional small radicals, thus resulting in the more recent, highly active quinolones sitafloxacin (13; DU 6859) [80][81][82][83][84], DK-507 k 14 [85,86] and olamufloxacin (15; HSR 903) [87][88][89][90]containing an (S)-3-amino-1-pyrrolidinyl radical in the 7-position, to which a cyclopropyl radical is attached spirocyclically in the 4-position. Due to the omission of the Cl substituent in sitafloxacin from DK-507 k, the latter's phototoxic potential was reduced.…”

“…The effectiveness of moxifloxacin (MIC 90 0.06-0.125 mg L -1 ) against methicillin-sensitive S. aureus (MSSA) is four-to eight-fold greater than that of ciprofloxacin, ofloxacin, and levofloxacin, although its in vitro activity against methicillinresistant S. aureus (MRSA) is less powerful (MIC 90 182,187,188], although its activity against specific bacteria is less powerful than that of ciprofloxacin [188]. When moxifloxacin was used in combination with cefepime or piperacillin/tazobactam against clinical isolates of K. pneumoniae, Enterobacter cloacae and Acinetobacter baumannii, an increase in bactericidal activity was obtained compared to that of the individual compounds; this was due to synergistic effects between the different compounds [189].…”

“…Moxifloxacin's MIC 90 ) [192][193][194]. A combination of moxifloxacin and isoniazid proved to be more effective in vivo than the individual compounds [195,196], whereas a combination with ethambutol was less effective [196].…”

“…Moxifloxacin is four times more effective than levofloxacin in suppressing the selection of resistant mutants of S. pneumoniae [251]. In a more recent study, other sequences were determined for MSSA based on the MIC 90 )] [252]. In order to prevent the development of a level of resistance which correlates with the quinolone concentration obtainable in vivo [219,232], this concentration should be higher than the MIC value (t > MIC) for as long a period as possible.…”

Studies on equilibrium of anthranilic acid in aqueous solutions and in two-phase systems: Aromatic solvent–water

“…These data do not allow prediction of the physicochemical properties and behavior of this acid in systems with other organic solvents. [14][15][16]. Their accurate determination is important for complete understanding the chemical behaviour and the biological activity of ampholytes.…”