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. 2016 Feb;23(6):520–577. doi: 10.2174/0929867323666151223095839

Table 11. Achillion isothiazoloquinolone SAR for MRSA (MIC) and cytotoxicity in Hep2 cells (CC50). Ciprofloxacin 15, moxifloxacin, and gemifloxacin 102 serve as reference compounds.

Compound R6 R7 X MRSAa
MIC
(µg/ml)
Hep2 cellsb
CC50 (µg/ml)c
[topo II
EC2 (µg/ml)]c,d
91 F CH 2 3
92 F COCH3 0.5 8 [32]
93 H COCH3 2 40
94 F CH 1 1
95 F COCH3 0.5 6 [15]
96 H COCH3 2 19
97 F COCH3 2 10
98 F COCH3 0.25 4
99 F COCH3 4 >43
100
ACH702
F COCH3 0.06 4
101 F COCH3 2 28
15
ciprofloxacin
F CH 32 >33 [>50]
12
moxifloxacin
F COCH3 2 >40 [>60]