The activities of @entity10127 compared to those of nine other agents was tested against a range of @entity114 -susceptible and -resistant pneumococci by agar dilution, microdilution, time-kill, and post-antibiotic effect (PAE) methods. Against 64 @entity114 -susceptible, 68 @entity114 -intermediate, and 75 @entity114 -resistant pneumococci (all @entity1536 susceptible), agar dilution MIC(50)s (MICs at which 50% of isolates are inhibited)/MIC(90)s (in micrograms per milliliter) were as follows: @entity10127 , 0.03/0.06; @entity2177 , 1.0/4.0; @entity800 , 1.0/2. 0; @entity18255 , 0.5/1.0; @entity43578 , 0.125/0.5; @entity36471 , 0. 125/0.25; @entity115 , 0.016/0.06 ( @entity114 -susceptible isolates), 0.125/1.0 ( @entity114 -intermediate isolates), and 2.0/4.0 ( @entity114 -resistant isolates); @entity2261 , 0.03/0.25 ( @entity114 -susceptible isolates), 0.5/2.0 ( @entity114 -intermediate isolates), and 8.0/16.0 ( @entity114 -resistant isolates); @entity4580 , 0.125/0.5 ( @entity114 -susceptible isolates), 0. 125/>128.0 ( @entity114 -intermediate isolates), and 4.0/>128.0 ( @entity114 -resistant isolates); and @entity4581 , 0.03/0.06 ( @entity114 -susceptible isolates), 0.03/32.0 ( @entity114 -intermediate isolates), and 2.0/>128.0 ( @entity114 -resistant isolates). Against 28 strains with @entity2177 MICs of >/=8 microg/ml, @entity10127 had the lowest MICs (0.03 to 1.0 microg/ml; MIC(90), 0.5 microg/ml), compared with MICs ranging between 0.25 and >32.0 microg/ml (MIC(90)s of 4.0 to >32.0 microg/ml) for other @entity5176 . Resistance in these 28 strains was associated with mutations in @entity30939 , gyrA, parE, and/or gyrB or efflux, with some strains having multiple resistance mechanisms. For 12 @entity114 -susceptible and -resistant pneumococcal strains (2 @entity1536 resistant), time-kill results showed that @entity800 at the MIC, @entity10127 and @entity18255 at two times the MIC, and @entity2177 , @entity43578 , and @entity36471 at four times the MIC were bactericidal for all strains after 24 h. @entity10127 was uniformly bactericidal after 24 h at </=0.5 microg/ml. Various degrees of 90 and 99% killing by all @entity5176 were detected after 3 h. @entity10127 and @entity36471 were both bactericidal at two times the MIC for the two @entity1536 -resistant pneumococci. @entity115 at two times the MIC and @entity2261 at four times the MIC were uniformly bactericidal after 24 h, with some degree of killing at earlier time points. @entity7187 gave slower killing against the seven susceptible strains tested, with 99.9% killing of all strains at two to four times the MIC after 24 h. PAEs for five @entity1536 -susceptible strains were similar (0.3 to 3.0 h) for all @entity5176 , and significant @entity1536 PAEs were found for the @entity1536 -resistant strain.

Antipneumococcal activities of XXXX compared to those of nine other agents.

@entity2261 :: ('MESH:D002444', 'Chemical') :: ['cefuroxime'] @entity30939 :: ('23113', 'Gene') :: ['parC'] @entity10127 :: ('MESH:C103274', 'Chemical') :: ['Gemifloxacin', 'gemifloxacin'] @entity18255 :: ('MESH:C061363', 'Chemical') :: ['sparfloxacin'] @entity115 :: ('MESH:D000658', 'Chemical') :: ['Amoxicillin', 'amoxicillin'] @entity5176 :: ('MESH:D015363', 'Chemical') :: ['quinolones'] @entity114 :: ('MESH:D010406', 'Chemical') :: ['penicillin'] @entity43578 :: ('MESH:C075375', 'Chemical') :: ['grepafloxacin'] @entity4581 :: ('MESH:D017291', 'Chemical') :: ['clarithromycin'] @entity2177 :: ('MESH:D002939', 'Chemical') :: ['ciprofloxacin'] @entity4580 :: ('MESH:D017963', 'Chemical') :: ['azithromycin'] @entity7187 :: ('MESH:D018942', 'Chemical') :: ['Macrolides'] @entity800 :: ('MESH:D015242', 'Chemical') :: ['levofloxacin'] @entity36471 :: ('MESH:C080163', 'Chemical') :: ['trovafloxacin'] @entity1536 :: ('CHEBI:23765', 'Chemical') :: ['quinolone']
@entity10127 :: (MESH:C103274,Chemical) :: ['gemifloxacin']
