Table 2. MRC and GI50 Values for the Substitutions of Indoline Aromatic Ring.
entry | compd | R1 | R2 | R3 | R4 | amox/clava,b | cefazolina,b | meropenema,c | GI50d |
---|---|---|---|---|---|---|---|---|---|
1 | 1 | H | Br | H | H | 4 | 4 | 4 | 17.1 |
2 | 6a | H | Cl | H | H | 8 | 4 | 8 | 35 |
3 | 6b | H | Me | H | H | 16 | 16 | 32 | – |
4 | 6c | H | MeO | H | H | >32 | >32 | >32 | – |
5 | 6d | H | F | H | H | 16 | 16 | 16 | – |
6 | 6e | H | H | H | H | 16 | 16 | 16 | – |
7 | 6f | H | H | phenylene | >32 | >32 | >32 | – | |
8 | 6g | H | H | H | Br | >32 | 32 | 8 | – |
9 | 6h | H | H | Br | H | 16 | 16 | 16 | – |
10 | 6i | Br | H | H | H | 32 | 16 | 16 | – |
11 | 6j | H | Cl | H | F | 16 | 16 | 32 | – |
12 | 6k | H | Cl | H | Cl | 4 | 4 | 4 | 13.6 |
13 | 6l | H | Br | H | F | 2 | 4 | 4 | 18.1 |
MRC values are in μg/mL.
MRSA ATCC BAA-44.
MRSA ATCC 33592.
HeLa cells; GI50 values are in μg/mL.