Table 1. Activity of top 27 active hits with better activity than the current Lyme disease antibiotics against stationary-phase B. burgdorferi persisters a.
| Drugs (50 μM) | Residual viable cellsb | Residual viable cellsc | Ratio of green/red fluoresce | |||
|---|---|---|---|---|---|---|
| Primary screening | Rescreening | Rescreening | P-valued | |||
| Control | 93% | 94% | 8.67 | 8.38 | 8.59 | - |
| Amoxicilline | 76% | 76% | 7.98 | 7.86 | 7.82 | 1.000000 |
| Doxycyclinee | 75% | 67% | 7.62 | 7.35 | 7.58 | 0.233596 |
| Penicillin Ge | 75% | 68% | 7.41 | 7.68 | 7.92 | 0.699416 |
| Tetracyclinee | 54% | 50% | 7.59 | 6.14 | 7.18 | 0.102366 |
| Ceftriaxonee | 50% | 44% | 6.74 | 6.89 | 6.78 | 0.000182 |
| Cefuroximee | 49% | 43% | 6.59 | 6.84 | 6.67 | 0.000317 |
| Clarithromycine | 70% | 65% | 7.70 | 7.36 | 7.59 | 0.038775 |
| Azithromycine | 77% | 80% | 8.33 | 8.10 | 7.92 | 0.071492 |
| Daptomycin | 35% | 28% | 6.10 | 6.20 | 6.09 | 0.000008 |
| Clofazimine | 45% | 32% | 6.56 | 6.23 | 6.02 | 0.000599 |
| Cefoperazone | 37% | 34% | 6.54 | 6.32 | 6.23 | 0.000126 |
| Carbomycin | 41% | 37% | 6.37 | 6.81 | 6.32 | 0.001045 |
| Vancomycin | 48% | 38% | 6.65 | 6.58 | 6.37 | 0.000152 |
| Cephalothin | 49% | 40% | 6.74 | 6.49 | 6.55 | 0.000133 |
| Cefotiam | 42% | 43% | 6.41 | 7.55 | 6.21 | 0.000503 |
| Cefmetazole | - | 43% | 6.80 | 7.38 | 6.00 | 0.045064 |
| Cefepime | - | 44% | 6.67 | 7.16 | 6.45 | 0.006368 |
| Amodiaquin | - | 45% | 6.79 | 6.44 | 6.85 | 0.000946 |
| Streptomycin | - | 45% | 6.72 | 6.93 | 6.76 | 0.000175 |
| Ticarcillin | - | 46% | 6.82 | 6.72 | 6.93 | 0.000163 |
| Cefonicid | - | 46% | 6.86 | 7.54 | 6.07 | 0.067661 |
| Piperacillin-tazobactam | 47% | 47% | 7.18 | 6.47 | 6.98 | 0.009594 |
| Cefdinir | - | 48% | 6.88 | 7.51 | 6.29 | 0.049107 |
| Ceforanide | - | 48% | 6.89 | 7.49 | 6.33 | 0.043847 |
| Cefmenoxime | - | 48% | 6.82 | 7.59 | 6.32 | 0.058674 |
| Bismuth | - | 48% | 6.94 | 6.82 | 6.92 | 0.000082 |
| Ceftizoxime | - | 49% | 6.94 | 6.83 | 7.03 | 0.000223 |
| Ceftibuten | 51% | 49% | 6.81 | 6.78 | 7.27 | 0.004888 |
| Amphotericin B | - | 50% | 7.14 | 6.88 | 6.87 | 0.000783 |
| Cefamandole | - | 50% | 6.71 | 7.73 | 6.52 | 0.076304 |
| Quinine hydrobromide | - | 50% | 7.00 | 6.85 | 6.88 | 0.000124 |
| Cyclacillin | 51% | 53% | 6.81 | 6.88 | 7.64 | 0.045210 |
| Colistin | 50% | 54% | 7.15 | 7.26 | 7.23 | 0.000319 |
| Sulfameter | 54% | 7.13 | 7.46 | 6.98 | 0.009635 | |
| Tigecycline | 58% | 51% | 6.98 | 7.06 | 6.96 | 0.001557 |
a
Stationary-phase B. burgdorferi (7-day old) cells were treated with drugs for 7 days. The line above clarithromycin refers to antibiotics used to treat Lyme disease.
b
Residual viable B. burgdorferi was assayed by epifluorescence microscope counting.
c
Residual viable B. burgdorferi was calculated according to the regression equation and ratio of Green/Red fluorescence obtained by SYBR Green I/PI assay.
d
P-values of the standard t-test for the treated group versus a control group treated with amoxicillin, which is known to have poor activity against stationary-phase persisters.
e
Currently recommended antibiotics for Lyme disease.5