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. Author manuscript; available in PMC: 2012 Aug 1.
Published in final edited form as: Bioorg Med Chem Lett. 2011 Jun 6;21(15):4585–4588. doi: 10.1016/j.bmcl.2011.05.112

Table 1.

MIC of C-2 and C-3 modified quinolones in E. coli and M. smegmatis.

Compound C-2 C-3 C-7 Bacterial Strain (MIC μg/mL)
E. colia E. coli tolCb M. smegmatisc
Ciprofloxacin H CO2H Piperazinyl 0.04 0.008 0.156
13 H H Piperazinyl 50 1.56 6.25
Ulifloxacin Thiazetidine CO2H Piperazinyl 0.062 0.016 3.13
15 Thiazetidine H Piperazinyl >200 200 200
Moxifloxacin H CO2H octahydropyrrolopyridinyl 0.156 0.004 0.08
11 H H octahydropyrrolopyridinyl >200 100 >200
7a S-ethyl CO2H Piperazinyl 200 12.5 >200
7b S-ethyl CO2H octahydropyrrolopyridinyl >50 >50 50
9a S-ethyl H Piperazinyl >50 25 >50
9b S-ethyl H octahydropyrrolopyridinyl >200 100 >200
9c S-isopropyl H Piperazinyl >50 >50 >50
9d S-isopropyl H octahydropyrrolopyridinyl >50 50 50
a

KD65

b

KD1397

c

KD1163