Table 1.
MIC and MBC values for carvacrol (parent compound) and its semi-synthetic derivatives (1–46) against nine strains of H. pylori. Antibiotic susceptibility is reported for each H. pylori strain.
|
H. pylori Strains MIC/MBC (µg/mL) | |||||||||
|---|---|---|---|---|---|---|---|---|---|
| F4 | 190 | 23 | 110 R | NCTC 11637 | F1 | F34/497 | F40/499 | F40/442 | |
| Carvacrol | 64/64 | 64/64 | 64/64 | 64/64 | 64/64 | 64/64 | 16/32 | 32/64 | 32/64 |
| 1 | 128/128 | >128/>128 | >128/>128 | 128/128 | >128/>128 | 128/128 | 128/128 | 64/64 | 64/64 |
| 2 | 64/64 | 64/128 | >128/>128 | 64/64 | 128/>128 | 64/64 | 32/64 | 32/64 | 64/64 |
| 3 | 64/128 | 64/64 | 128/>128 | 64/64 | 64/64 | 64/64 | 32/64 | 64/64 | 64/64 |
| 4 | 128/128 | 128/128 | 128/128 | 128/128 | 128/128 | 128/128 | 128/128 | 128/128 | 128/128 |
| 5 | 64/64 | 64/64 | 64/64 | 64/64 | 128/128 | 64/64 | 64/64 | 64/64 | 64/64 |
| 6 | 16/32 | 32/32 | 32/64 | 64/128 | 64/64 | 32/32 | 32/32 | 16/16 | 32/32 |
| 7 | 32/32 | 32/64 | 64/128 | 64/128 | 64/64 | 32/32 | 32/32 | 64/64 | 64/64 |
| 8 | 64/64 | 64/64 | 64/64 | 64/128 | 64/64 | 64/64 | 64/64 | 64/64 | 64/64 |
| 9 | 8/8 | 32/32 | 32/64 | 32/32 | 32/32 | 16/16 | 8/8 | 16/16 | 16/16 |
| 10 | 128/128 | 128/128 | 128/128 | 128/128 | 128/128 | 128/128 | 128/128 | 128/128 | 128/128 |
| 11 | 128/128 | 128/128 | 128/128 | 128/128 | 128/128 | 128/128 | 128/128 | 128/128 | 128/128 |
| 12 | 64/64 | 32/32 | 128/128 | 64/64 | 64/64 | 64/64 | 64/64 | 32/64 | 64/64 |
| 13 | >128/>128 | >128/>128 | >128/>128 | >128/>128 | >128/>128 | >128/>128 | 128/128 | 128/128 | 128/128 |
| 14 | 64/64 | 64/64 | 64/64 | 64/64 | 64/64 | 64/64 | 64/64 | 64/64 | 64/64 |
| 15 | 64/128 | 64/64 | 32/32 | 64/64 | 64/64 | 32/64 | 32/32 | 32/32 | 32/32 |
| 16 | 8/16 | 8/16 | 32/32 | 8/8 | 32/32 | 4/8 | 2/2 | 8/8 | 4/8 |
| 17 | 32/32 | 32/32 | 16/16 | 32/32 | 32/32 | 16/16 | 8/32 | 16/16 | 16/16 |
| 18 | 32/32 | 32/64 | 32/32 | 64/128 | 32/64 | 16/32 | 16/16 | 16/16 | 16/16 |
| 19 | 32/64 | >128/>128 | >128/>128 | >128/>128 | 128/128 | 32/32 | 16/32 | 64/128 | 64/128 |
| 20 | 16/32 | 128/128 | 32/64 | 128/>128 | 64/64 | 32/32 | 16/32 | 64/64 | 64/64 |
| 21 | 16/32 | 32/32 | 32/64 | 32/64 | 32/64 | 32/32 | 16/32 | 32/32 | 32/32 |
| 22 | >128/>128 | >128/>128 | >128/>128 | >128/>128 | >128/>128 | 128/>128 | >128/>128 | >128/>128 | >128/>128 |
| 23 | 64/64 | 32/32 | 64/64 | 32/64 | 64/64 | 64/64 | 64/64 | 32/32 | 32/64 |
| 24 | 32/32 | 64/128 | 32/32 | 64/64 | 64/128 | 32/32 | 128/128 | 32/32 | 32/32 |
| 25 | 64/64 | 32/32 | 64/64 | 64/64 | 64/64 | 64/64 | 32/64 | 32/64 | 32/64 |
| 26 | 32/32 | 32/32 | 32/32 | 32/32 | 32/64 | 16/16 | 32/64 | 16/16 | 16/16 |
| 27 | 32/64 | 32/32 | 64/64 | 32/32 | 64/64 | 32/64 | 32/32 | 32/32 | 32/32 |
| 28 | 16/16 | 16/16 | 32/64 | 16/32 | 16/32 | 8/8 | 32/64 | 8/8 | 8/16 |
| 29 | 16/64 | 32/64 | 64/64 | 64/64 | 64/64 | 64/64 | 16/32 | 64/64 | 16/32 |
| 30 | 32/64 | 64/128 | 64/128 | 64/128 | 64/128 | 64/64 | 32/32 | 32/64 | 32/64 |
| 31 | 32/32 | 16/32 | 32/64 | 16/16 | 64/64 | 16/32 | 64/64 | 8/16 | 16/32 |
| 32 | 16/32 | 64/64 | 64/64 | 64/64 | 32/64 | 32/32 | 16/16 | 32/64 | 16/32 |
| 33 | 8/8 | 4/4 | 8/8 | 4/4 | 4/4 | 8/8 | 8/8 | 8/8 | 8/8 |
| 34 | 8/8 | 4/4 | 4/4 | 4/8 | 4/4 | 4/4 | 4/4 | 4/4 | 4/4 |
| 35 | 4/8 | 16/16 | 32/64 | 16/16 | 32/64 | 4/4 | 2/2 | 16/16 | 16/16 |
| 36 | 8/16 | 4/4 | 8/8 | 8/8 | 8/8 | 8/8 | 8/8 | 8/8 | 8/8 |
| 37 | 32/64 | 64/64 | 64/64 | 64/64 | 64/64 | 32/64 | 32/32 | 64/64 | 32/64 |
| 38 | 8/8 | 4/4 | 8/8 | 4/4 | 8/8 | 4/4 | 2/2 | 8/8 | 8/8 |
| 39 | 2/2 | 4/4 | 2/2 | 4/4 | 2/2 | 2/2 | 2/2 | 2/2 | 2/2 |
| 40 | 8/8 | 8/16 | 8/16 | 8/16 | 8/16 | 4/4 | 4/4 | 4/4 | 4/4 |
| 41 | >128/>128 | >128/>128 | >128/>128 | >128/>128 | >128/>128 | >128/>128 | >128/>128 | >128/>128 | >128/>128 |
| 42 | 16/16 | 16/32 | 32/32 | 32/32 | 32/32 | 32/32 | 16/32 | 32/32 | 16/16 |
| 43 | 32/32 | 64/128 | 128/>128 | 128/>128 | 128/>128 | 32/32 | 64/128 | 32/32 | 32/32 |
| 44 | 32/32 | 32/32 | 32/32 | 32/32 | 32/32 | 32/32 | 32/32 | 32/32 | 32/32 |
| 45 | 32/32 | 32/128 | 64/>128 | 32/128 | 64/128 | 32/32 | 32/32 | 32/32 | 32/32 |
| 46 | 64/128 | 32/64 | 32/64 | 32/64 | 32/64 | 64/128 | 64/>128 | 32/64 | 64/128 |
| Antibiotic susceptibility | MTZ+ | MTZ− | MTZ− | MTZ+ | MTZ+ | MTZ− | MTZ+ | MTZ+ | MTZ+ |
| CLR+ | CLR− | CLR− | CLR− | CLR− | CLR+ | CLR+ | CLR+ | CLR− | |
| AMX− | AMX− | AMX− | AMX− | AMX− | AMX− | AMX− | AMX− | AMX− | |
MTZ+ = metronidazole resistant (MIC > 8 µg/mL); MTZ− = metronidazole susceptible (MIC ≤ 8 µg/mL); CLR+ = clarithromycin resistant (MIC > 0.25 µg/mL); CLR− = clarithromycin susceptible (MIC ≤ 0.25 µg/mL); AMX+ = amoxicillin resistant (MIC > 0.125 µg/mL); AMX− = amoxicillin susceptible (MIC ≤ 0.125 µg/mL). Compounds selected for in vitro anti-proliferative activity assays against AGS cells are highlighted in grey.