Table 3. MRC and GI50 Values for 1 Analogues with Modifications on the Side Chain.
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 |
MRC values are in μg/mL.
MRSA ATCC BAA-44.
MRSA ATCC 33592.
HeLa cells; GI50 values are in μg/mL.