TABLE 4.

Structures of the quinolones tested and MICs  

Quinolone	Basea	Group atb:					Anti-MAI activity (μg/ml)c
		R1	R8	R5	R6	R7	Exper.	Calc.
Moxifloxacin	A	Cyclopropyl	-OCH3	H	F	Piperidino-pyrrolidinyl	0.2	0.7
Sparfloxacin	A	Cyclopropyl	F	NH2	F	3′,5′-Methylpiperazinyl	0.4	0.3
Gatifloxacin	A	Cyclopropyl	-OCH3	H	F	3′-Methylpiperazinyl	0.9	0.8
Temafloxacin	A	2,4-Difluorophenyl	H	H	F	3′-Methylpiperazinyl	1.0	0.8
Levofloxacin	A			H	F	4′-Methylpiperazinyl	2.1	4.0
Ofloxacin	A			H	F	4′-Methylpiperazinyl	2.5	4.0
Trovafloxacin	B	2,4-Difluorophenyl		H	F	Aza-bicyclohexanyl	2.7	1.7
Ciprofloxacin	A	Cyclopropyl	H	H	F	1-Piperazinyl	2.8	7.3
Lomefloxacin	A	-CH2CH3	F	H	F	3′-Methylpiperazinyl	4.5	4.9
Clinafloxacin	A	Cyclopropyl	Cl	H	F	3′-Aminopyrrolidinyl	5.0	3.1
Grepafloxacin	A	Cyclopropyl	H	CH3	F	3′-Methylpiperazinyl	5.4	1.8
Fleroxacin	A	-CH2CH2F	F	H	F	4′-Methylpiperazinyl	8.1	4.7
Pefloxacin	A	-CH2CH3	H	H	F	4′-Methylpiperazinyl	10.0	13.6
Norfloxacin	A	-CH2CH3	H	H	F	1-Piperazinyl	11.4	24.5
Enoxacin	B	-CH2CH3		H	F	1-Piperazinyl	13.7	27.7
Acrosoxacin	A	-CH2CH3	H	H	H	4-Pyridinyl	23.5	68.8
Rufloxacin	A			H	F	1-Piperazinyl	31.0	11.9
Irloxacin	A	-CH2CH3	H	H	F	1-Pyrrolyl	47.2	89.1
Pipemidic acid	C	-CH2CH3		H		1-Piperazinyl	>250.0	95.8
Flumequine	A			H	F	H	>250.0	82.1
Piromidic acid	C	-CH2CH3		H		1-Pyrrolidinyl	>250.0	330.9
Nalidixic acid	B	-CH2CH3		H	H	CH3	>250.0	462.5
Cinoxacin	D	-CH2CH3	H	H			>250.0	486.3
Oxolinic acid	A	-CH2CH3	H	H			>250.0	449.3

^aA, B, C, and D, basic nucleus quinoline, 1,8-naphtyridine, pyrido[2,3-d]pyrimidine, and 1,2-cinnoline, respectively. 

^bLevofloxacin R1 to R8, R1-CH(CH₃)CH₂O-R8; ofloxacin R1 to R8, R1-CH(CH₃)CH₂O-R8; rufloxacin R1 to R8, R1-CH₂CH₂S-R8; flumequine R1 to R8, R1-CH(CH₃)CH₂CH₂-R8; cinoxacin R6 to R7, R6-O-CH₂-O-R7; oxolinic acid R6 to R7, R6-O-CH₂-O-R7. 

^cExper., experimental; calc, calculated.