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. 2014 Apr 2;57(9):3803–3817. doi: 10.1021/jm500146g

Table 3. MRC and GI50 Values for 1 Analogues with Modifications on the Side Chain.

graphic file with name jm-2014-00146g_0008.jpg

entry compd R1 R2 amox/clava,b cefazolina,b meropenema,c GI50d
1 1 H SO2PhpCl 4 4 4 17.1
2 11a H H 32 32 32
3 11b F H >32 32 16 16.2
4 12a H TFA >32 >32 32
5 12b H COBu >32 >32 32
6 12c H COPhpCl >32 >32 >32
7 12d H SO2Ph 8 8 16
8 12e H SO2PhpMe >32 >32 >32
9 12f H SO2PhpF >32 >32 >32
10 12g H SO2PhpBr 4 4 8 40
11 12h H SO2PhpI 4 4 32 33
12 12i H SO2Ph3,4Cl 4 2 4 12.8
13 12j H SO2Ph2,4Cl 8 >32 4
14 12k H SO2PhpCN 16 8 16
15 12l H SO2PhpNHAc >32 >32 32
16 12m H SO25Py 32 32 32
17 12n H SO2PhpNO2 >32 >32 >32
18 12o H SO2PhpNH2 16 16 16
20 13a F SO2PhpOMe 8 4 8 49
21 13b F SO2PhpMe 4 4 4 22
22 13c F SO2PhpF 4 4 4 18.3
23 6l F SO2PhpCl 2 4 4 18.1
24 13d F SO2PhpBr 1 1 1 22
25 13e F SO2PhpI 4 2 4 19.6
26 13f F SO2Ph3,4Cl 4 4 4 31
27 13g F SO2PhpNHAc 32 32 16 32
28 13h F SO2PhpCN 8 4 4 17.0
29 13i F SO2PhpCF3 4 4 4 8.7
a

MRC values are in μg/mL.

b

MRSA ATCC BAA-44.

c

MRSA ATCC 33592.

d

HeLa cells; GI50 values are in μg/mL.