Table 1.

Frequencies of appearance of mutant strains by selection with gatifloxacin and its related compounds

Selecting quinoloneSubstitutions at the following positiona:Frequency at the following multiple of the MICb:
83′124816
GatifloxacinOCH3 CH3 3.7 × 10−9 <2.4 × 10−9 <2.4 × 10−9 <2.4 × 10−9 <2.4 × 10−9
AM-1121HCH3 >2.4 × 10−6 >2.4 × 10−6 <2.4 × 10−9 <2.4 × 10−9 <2.4 × 10−9
AM-1147OCH3 H<2.4 × 10−9 <2.4 × 10−9 <2.4 × 10−9 <2.4 × 10−9 <2.4 × 10−9
CiprofloxacinHH>2.4 × 10−6 >2.4 × 10−6 <2.4 × 10−9 <2.4 × 10−9 <2.4 × 10−9
  • a 8, position C-8 of the quinolone ring; 3′, position 3′ of the C-7 piperazinyl moiety.

  • b The reproducibility of the frequency was confirmed by repeated experiments.