Table 1.
In vitro activities against G+ bacteria of the aimed compounds.
| NO. | R | Staphylococcus epidermidis (MIC a) | Staphylococcus.aureus (MIC) | Enterococci.faecalis (MIC) | Enterococci.faecium (MIC) | ||||||
|---|---|---|---|---|---|---|---|---|---|---|---|
| ATCC 12228 MSSE b |
12-6 MSSE |
ATCC 29213 MSSA c |
ATCC 33591 MRSA d |
15 MSSA |
12-28 MSSA |
ATCC 29212 VSE e |
ATCC 51299 VRE f |
ATCC 700221 VRE |
12-3 VSE |
||
| 1 |
|
16 (49.4) | 8 (24.7) | 16 (49.4) | 16 (49.4) | 16 (49.4) | 8 (24.7) | 8 (24.7) | 8 (24.7) | 8 (24.7) | 8 (24.7) |
| 2 | - | 8 (44.7) | 16 (89.4) | 8 (44.7) | 16 (89.4) | 8 (44.7) | 8 (44.7) | 16 (89.4) | 16 (89.4) | 16 (89.4) | 8 (44.7) |
| 4a | CH3 | 32 (136) | 32 (136) | 32 (136) | 32 (136) | 32 (136) | 32 (136) | 32 (136) | 32 (136) | 32 (136) | 32 (136) |
| 4b | CH3CH2CH2- | 32 (122) | 32 (122) | 32 (122) | 32 (122) | 32 (122) | 32 (122) | 32 (122) | 32 (122) | 32 (122) | 32 (122) |
| 4c | (CH3)2CH- | 32 (122) | 32 (122) | 32 (122) | 32 (122) | 32 (122) | 32 (122) | 32 (122) | >64 (>243) | >64 (>243) | 32 (122) |
| 4d | CH2=CHCH2- | 16 (61.3) | 16 (61.3) | 16 (61.3) | 16 (61.3) | 16 (61.3) | 16 (61.3) | 16 (61.3) | 16 (61.3) | 32 (123) | 16 (61.3) |
| 4e | CH≡CCH2- | 16 (61.8) | 16 (61.8) | 32 (124) | 16 (61.8) | 32 (124) | 32 (124) | 16 (61.8) | 16 (61.8) | 16 (61.8) | 16 (61.8) |
| 4f | (CH3)2NCH2CH2- | 32 (110) | 32 (110) | 32 (110) | 32 (110) | 32 (110) | 64 (219) | 32 (110) | 32 (110) | 64 (219) | 64 (219) |
| 4g | CNCH2CH2- | 8 (29.2) | 8 (29.2) | 8 (29.2) | 8 (29.2) | 16 (58.4) | 8 (29.2) | 8 (29.2) | 8 (29.2) | 16 (58.4) | 8 (29.2) |
| 4h | CH3OCOCH2- | 8 (27.3) | 8 (27.3) | 8 (27.3) | 8 (27.3) | 8 (27.3) | 8 (27.3) | 16 (54.6) | 16 (54.6) | 8 (27.3) | 16 (54.6) |
| 4i | PhCH2OCOCH2- | >64 (>173) | >64 (>173) | >64 (>173) | >64 (>173) | >64 (>173) | >64 (>173) | >64 (>173) | >64 (>173) | >64 (>173) | >64 (>173) |
| 4j |
|
16 (61.3) | 16 (61.3) | 16 (61.3) | 16 (61.3) | 16 (61.3) | 16 (61.3) | 16 (61.3) | 16 (61.3) | 16 (61.3) | 32 (123) |
| 4k |
|
16 (50.3) | 16 (50.3) | 64 (201) | 64 (201) | 64 (201) | 64 (201) | 32 (101) | 64 (201) | 64 (201) | 64 (201) |
| 4l |
|
64 (201) | 64 (201) | 64 (201) | 64 (201) | 128 (401) | 64 (201) | 64 (201) | 128 (401) | 128 (401) | 128 (401) |
| 4m |
|
64 (184) | 64 (184) | 64 (184) | 64 (184) | 64 (184) | 64 (184) | 64 (184) | >64 (>184) | >64 (>184) | >64 (>184) |
| 5a |
|
32 (122) | 32 (122) | 32 (122) | 32 (122) | 32 (122) | 64 (243) | 32 (122) | 32 (122) | 64 (243) | 64 (243) |
| 5b |
|
16 (57.3) | 16 (57.3) | 16 (57.3) | 16 (57.3) | 16 (57.3) | 16 (57.3) | 16 (57.3) | 16 (57.3) | 16 (57.3) | >128 (>459) |
| 5c |
|
128 (438) | 128 (438) | >128 (>438) | >128 (>438) | >128 (>438) | >128 (>438) | 128 (438) | 128 (438) | 128 (438) | >128 (>438) |
| 5d |
|
4 (7.65) | 16 (30.6) | 4 (7.65) | 8 (15.3) | 4 (7.65) | 4 (7.65) | 8 (7.65) | 16 (15.3) | >128 (>245) | 0.5 (0.956) |
| 6a |
|
128 (263) | 128 (263) | 128 (263) | 128 (263) | 128 (263) | 128 (263) | 128 (263) | 128 (263) | 128 (263) | 128 (263) |
| 6b |
|
128 (222) | 128 (222) | 128 (222) | 128 (222) | 128 (222) | 128 (222) | 128 (222) | 128 (222) | 128 (222) | 128 (222) |
| CPFX | - | 0.125 (0.378) | 0.5 (1.51) | 0.25 (0.755) | 0.25 (0.755) | 0.125 (0.378) | 0.25 (0.755) | 0.5 (1.51) | 0.5 (1.51) | >128 (>387) | 64 (193) |
a MIC was determined by agar dilution. MIC unit: μg/mL(μM). b MSSE, methicillin-sensitive Staphylococcus epidermidis; c MSSA, methicillin-sensitive Staphylococcus aureus; d MRSA, methicillin-resistant Staphylococcus aureus; e VSE, vancomycin-sensitive Enterococci; f VRE, vancomycin-resistant Enterococci.