TABLE 2.

Antibacterial activities of DX-619 and reference compounds against gram-negative bacteria

Organism (no. of strains) and compound	MIC (μg/ml)
	Range	50%	90%
Haemophilus influenzae
Ampicillin susceptible (20)
DX-619	≦0.004-0.008	≦0.004	≦0.004
Levofloxacin	0.008-0.015	0.015	0.015
Sitafloxacin	≦0.004	≦0.004	≦0.004
Ciprofloxacin	≦0.004-0.015	0.008	0.008
Moxifloxacin	≦0.004-0.015	0.008	0.015
Gatifloxacin	≦0.004-0.015	0.008	0.008
Garenoxacin	≦0.004-0.008	≦0.004	0.008
Imipenem	0.06-4	0.5	1
Ceftazidime	0.06-0.5	0.12	0.25
Cefaclor	1-8	2	4
Ampicillin	0.12-0.5	0.25	0.5
β-Lactamase positive, ampicillin resistant (21)
DX-619	≦0.004-0.008	≦0.004	≦0.004
Levofloxacin	≦0.004-0.015	0.015	0.015
Sitafloxacin	≦0.004	≦0.004	≦0.004
Ciprofloxacin	≦0.004-0.015	0.008	0.008
Moxifloxacin	≦0.004-0.03	0.015	0.015
Gatifloxacin	≦0.004-0.015	0.008	0.008
Garenoxacin	≦0.004-0.015	≦0.004	0.008
Imipenem	0.25-4	1	2
Ceftazidime	0.06-0.5	0.12	0.5
Cefaclor	1-32	8	16
Ampicillin	4-128	16	32
β-Lactamase negative, ampicillin intermediate and resistant (25)
DX-619	≦0.004-0.015	≦0.004	0.015
Levofloxacin	0.008-0.015	0.015	0.015
Sitafloxacin	≦0.004	≦0.004	≦0.004
Ciprofloxacin	0.008-0.015	0.008	0.015
Moxifloxacin	0.008-0.03	0.015	0.03
Gatifloxacin	≦0.004-0.015	0.008	0.015
Garenoxacin	≦0.004-0.015	0.008	0.015
Imipenem	0.25-8	4	8
Ceftazidime	0.12-1	0.5	0.5
Cefaclor	8-128	64	128
Ampicillin	2-8	4	8
Moraxella catarrhalis (48)
DX-619	0.008-0.06	0.015	0.03
Levofloxacin	0.03-0.06	0.03	0.06
Sitafloxacin	≦0.004-0.015	0.008	0.015
Ciprofloxacin	0.03-0.06	0.03	0.06
Moxifloxacin	0.03-0.12	0.06	0.06
Gatifloxacin	0.03-0.06	0.03	0.06
Garenoxacin	0.008-0.03	0.015	0.03
Imipenem	0.12-2	1	1
Ceftazidime	0.12->32	0.5	2
Ampicillin	0.25-8	4	8
Escherichia coli (48)
DX-619	0.015-8	0.03	1
Levofloxacin	0.015-32	0.06	4
Sitafloxacin	≦0.004-2	0.015	0.5
Ciprofloxacin	≦0.004-64	0.015	4
Moxifloxacin	0.015-32	0.06	8
Gatifloxacin	0.008-16	0.03	4
Garenoxacin	0.015-64	0.06	8
Imipenem	0.06-0.5	0.12	0.25
Ceftazidime	0.06-8	0.25	0.5
Ampicillin	1->128	4	>128
Klebsiella pneumoniae (49)
DX-619	0.03-1	0.06	0.12
Levofloxacin	0.015-2	0.06	0.12
Sitafloxacin	≦0.004-0.5	0.03	0.03
Ciprofloxacin	≦0.004-0.5	0.03	0.06
Moxifloxacin	0.06-2	0.12	0.25
Gatifloxacin	0.015-2	0.06	0.12
Garenoxacin	0.06-2	0.12	0.25
Imipenem	0.12-0.5	0.12	0.25
Ceftazidime	0.06-1	0.12	0.25
Ampicillin	1->128	32	32
Enterobacter spp. (26)
DX-619	0.03-2	0.06	0.5
Levofloxacin	0.03-2	0.06	0.5
Sitafloxacin	0.015-0.5	0.015	0.12
Ciprofloxacin	0.008-2	0.015	0.25
Moxifloxacin	0.03-4	0.06	0.5
Gatifloxacin	0.03-2	0.03	0.5
Garenoxacin	0.03-8	0.12	1
Imipenem	0.12-1	0.25	1
Ceftazidime	0.12->128	0.25	64
Citrobacter spp. (26)
DX-619	0.03-4	0.25	1
Levofloxacin	0.015-4	0.12	0.5
Sitafloxacin	0.008-2	0.06	0.5
Ciprofloxacin	0.008-2	0.03	0.25
Moxifloxacin	0.03-8	0.25	2
Gatifloxacin	0.015-4	0.12	1
Garenoxacin	0.03-16	0.5	4
Imipenem	0.25-1	0.5	1
Ceftazidime	0.12->128	1	128
Salmonella spp. (26)
DX-619	0.06-0.25	0.06	0.06
Levofloxacin	0.03-0.12	0.06	0.06
Sitafloxacin	0.015-0.12	0.015	0.015
Ciprofloxacin	0.015-0.12	0.015	0.015
Moxifloxacin	0.06-0.5	0.12	0.12
Gatifloxacin	0.03-0.25	0.06	0.06
Garenoxacin	0.06-0.5	0.06	0.12
Imipenem	0.12-0.25	0.25	0.25
Ceftazidime	0.25-0.5	0.25	0.5
Proteus mirabilis (26)
DX-619	0.06-4	0.12	2
Levofloxacin	0.03-8	0.06	2
Sitafloxacin	0.015-1	0.03	0.25
Ciprofloxacin	0.015-4	0.03	1
Moxifloxacin	0.25-32	0.5	8
Gatifloxacin	0.06-16	0.12	2
Garenoxacin	0.12-32	0.5	16
Imipenem	0.25-4	1	2
Ceftazidime	0.03-0.25	0.06	0.12
Indole-positive Proteus (25)
DX-619	0.03-8	0.12	0.5
Levofloxacin	0.015-4	0.06	0.25
Sitafloxacin	≦0.004-1	0.015	0.06
Ciprofloxacin	≦0.004-4	0.015	0.06
Moxifloxacin	0.06-32	0.25	0.5
Gatifloxacin	0.03-8	0.12	0.5
Garenoxacin	0.12-128	0.25	2
Imipenem	0.25-4	2	4
Ceftazidime	0.06-16	0.12	0.25
Serratia marcescens (26)
DX-619	0.12-8	0.5	2
Levofloxacin	0.06-8	0.25	2
Sitafloxacin	0.03-1	0.12	0.5
Ciprofloxacin	0.03-8	0.06	2
Moxifloxacin	0.12-16	0.5	4 ?xpp Tr>  Gatifloxacin	0.12-8	0.25	2
Garenoxacin	0.5-64	1	4
Imipenem	0.5-2	1	1
Ceftazidime	0.12-16	0.5	4
Pseudomonas aeruginosa
Ciprofloxacin susceptible (51)
DX-619	0.25-2	1	1
Levofloxacin	0.25-2	0.5	1
Sitafloxacin	0.03-0.25	0.12	0.25
Ciprofloxacin	0.06-0.5	0.12	0.25
Moxifloxacin	0.5-4	2	2
Gatifloxacin	0.25-2	1	1
Garenoxacin	0.25-4	1	2
Imipenem	0.5-32	2	16
Ceftazidime	0.5-128	2	4
Ciprofloxacin intermediate and    resistant (52)
DX-619	2->128	16	64
Levofloxacin	4->128	32	>128
Sitafloxacin	0.5-32	4	16
Ciprofloxacin	2->64	16	64
Moxifloxacin	8->128	64	>128
Gatifloxacin	4->128	32	64
Garenoxacin	8->128	64	>128
Imipenem	0.5->128	16	128
Ceftazidime	1->128	16	>128
Stenotrophomonas maltophilia (20)
DX-619	0.12-2	0.5	2
Levofloxacin	0.06-4	1	4
Sitafloxacin	0.03-0.5	0.12	0.5
Ciprofloxacin	0.015-8	2	4
Moxifloxacin	0.12-2	0.5	2
Gatifloxacin	0.12-4	1	2
Garenoxacin	0.25-8	2	8
Imipenem	2->128	>128	>128
Ceftazidime	2-128	32	128
Acinetobacter spp. (26)
DX-619	0.03-1	0.03	0.12
Levofloxacin	0.06-4	0.12
Sitafloxacin	0.015-1	0.03	0.12
Ciprofloxacin	0.06-8	0.12	0.5
Moxifloxacin	0.03-2	0.06	0.5
Gatifloxacin	0.03-2	0.06	0.25
Garenoxacin	0.015-2	0.03	0.12
Imipenem	0.12-0.5	0.25	0.5
Ceftazidime	1-16	4	8
Neisseria gonorrhoeae
Ciprofloxacin susceptible (23)
DX-619	≦0.004-0.015	≦0.004	0.015
Levofloxacin	≦0.004-0.12	0.008	0.06
Sitafloxacin	≦0.004	≦0.004	≦0.004
Ciprofloxacin	≦0.004-0.06	0.008	0.06
Moxifloxacin	≦0.004-0.06	0.008	0.06
Gatifloxacin	≦0.004-0.03	0.008	0.03
Garenoxacin	≦0.004-0.03	≦0.004	0.015
Imipenem	0.03-2	0.06	0.25
Ceftazidime	0.008-0.25	0.06	0.12
Benzylpenicillin	0.06-1	0.12	0.25
Ciprofloxacin resistant (26)
DX-619	0.25-2	0.5	1
Levofloxacin	4-16	8	16
Sitafloxacin	0.12-0.5	0.25	0.5
Ciprofloxacin	4-32	16	32
Moxifloxacin	2-8	4	8
Gatifloxacin	1-4	2	4
Garenoxacin	1-8	2	4
Imipenem	0.03-2	1	2
Ceftazidime	0.06-1	0.5	1
Benzylpenicillin	0.06-4	2	4
Bacteroides fragilis (20)
DX-619	0.06-0.5	0.06	0.5
Levofloxacin	1-32	1	32
Sitafloxacin	0.03-0.5	0.06	0.25
Ciprofloxacin	4-64	4	64
Moxifloxacin	0.25-8	0.25	4
Gatifloxacin	0.25-8	0.5	8
Garenoxacin	0.12-2	0.12	2
Imipenem	0.06-2	0.12	1
Ceftazidime	4->128	32	>128
Metronidazole	0.25-1	0.5	1
Clindamycin	0.06->128	0.25	>128