Table 1.
Compounds with greater than 80% growth inhibition of M. tuberculosis at 5 μM.
| i. WHO recommended drugs | |||
|---|---|---|---|
|
| |||
| Compound | Current Use | Route of delivery |
Anti-tuberculosis MIC (μM) |
| Rifampicin (Rifampin) | Antibacterial (First-line anti- tuberculosis agent) |
Oral | 0.02 |
| 3-formyl Rifamycin | Antibacterial (Anti-tuberculosis agent) |
Oral | 0.08 |
|
Isoniazid (Isonicotinic
acid hydrazide) |
Antibacterial (First-line anti- tuberculosis agent) |
Oral | 0.16 |
| Moxifloxacin HCl | Antibiotic (Fluoroquinolone – anti-tuberculosis agent) |
Oral | 0.16 |
| Amikacin | Antibiotic (Anti-tuberculosis agent) |
Intravenous | 0.31 |
| Ofloxacin | Antibiotic (Fluoroquinolone – anti-tuberculosis agent) |
Oral | 0.63 |
| Clofazimine | Antibacterial (Anti-tuberculosis agent) |
Oral | 1.25 |
| Gatifloxacin | Antibiotic (Fluoroquinolone – anti-tuberculosis agent) |
Oral | 1.25 |
| Levofloxacin HCl | Antibiotic (Fluoroquinolone – anti-tuberculosis agent) |
Oral | 1.25 |
| Ofloxacin | Antibiotic (Fluoroquinolone – anti-tuberculosis agent) |
Oral | 2.5 |
| Protionamide | Antibacterial (Second-line anti-tuberculosis agent) |
Oral | >5uM |
| Rifamycin sv | Antibacterial (First-line anti- tuberculosis agent) |
Oral | >5uM |
|
Thiacetazone
(Amithiozone) |
Antibacterial (Second-line anti-tuberculosis agent) |
Oral | >5uM |
| p-Aminosalicylic acid | Antibacterial (Second-line anti-tuberculosis agent) |
Oral | >5uM |
| Kanamycin B sulfate salt | Antibiotic (Anti-tuberculosis agent) |
Intravenous | >5uM |
| ii. Anti-tuberculosis drugs – compounds with known anti-mycobacterial activity | |||
|---|---|---|---|
|
| |||
| Compound | Current Use | Route of delivery |
Anti-tuberculosis MIC (μM) |
| Thiostrepton | Antibiotic | Topical | 0.08 |
| Rifaximin | Antibiotic | Oral (Non- systemic) |
0.08 |
| Sparfloxacin32, 33 | Antibiotic (Fluoroquinolone) | Oral | 0.08 |
| Doxycycline hyclate | Antibiotic (Anti-mycobacterial agent) |
Oral | 0.16 |
| Clinafloxacin HCl 34 | Antibiotic (Fluoroquinolone) | Oral | 0.31 |
|
Minocycline
hydrochloride salt 35 |
Antibiotic (Anti-mycobacterial agent) |
Oral | 0.31 |
| Aconiazide 36 | Antibacterial (Anti-tuberculosis agent) |
Oral | 0.63 |
| Doxycycline | Antibiotic (Anti-mycobacterial agent) |
Oral | 0.63 |
|
Vancomycin HCl
hydrate 35 |
Antibiotic (Agent) | Oral | 0.63 |
| Enrofloxacin | Antibiotic (Fluoroquinolone) | Oral | 1.25 |
| Tetracycline 37 | Antibiotic | Oral | 1.25 |
| Fleroxacin 38 | Antibiotic (Fluoroquinolone) | Oral | 2.5 |
| Tosufloxacin | Antibiotic (Fluoroquinolone) | Oral | 2.5 |
| Lomefloxacin33, 39 | Antibiotic (Fluoroquinolone) | Oral | 5 |
| Nialamide21, 22 | Antidepressant | Oral | 5 |
| Pazufloxacin 40 | Antibiotic (Fluoroquinolone) | Oral | 5 |
| Sarafloxacin HCl 41 | Antibiotic (Fluoroquinolone) | Oral | 5 |
|
Chlorhexidine
gluconate 42 |
Antiseptic | Topical | 5 |
| Methylene blue hydrate 43 | Antimethemoglobinemic | Intravenous | >5uM |
| Miconazole 44 | Antifungal | Topical | >5uM |
| Sulfathiazole | Antibiotic (Anti-mycobacterial agent) |
Oral | >5uM |
| iii. Novel anti-tuberculosis drugs | |||
|---|---|---|---|
|
| |||
| Compound | Current Use | Route of delivery |
Anti-tuberculosis MIC (μM) |
| Pyrvinium pamoate | Antihelmintic (Agent) | Oral | 0.31 |
| Bismuth subnitrate | Antacid | Oral | 2.5 |
|
Cefmenoxime
hydrochloride |
Antibiotic | Intravenous | 2.5 |
|
Pyrithione zinc (1-
Hydroxypyridine-2-thione Zinc Salt) |
Antibacterial | Topical | 2.5 |
|
Cetalkonium chloride
(Benzyldimethylhexadecyl ammonium chloride) |
Antibacterial | Topical | 5 |
| Hexadimethrine bromide | Antidote | Intravenous | 5 |
|
Methylbenzethonium
chloride |
Antiseptic | Topical | 5 |
| Primaquine | Antimalarial | Oral | 5 |
|
Protamine chloride, grade
V |
Antidote | Intravenous | 5 |
| Thonzonium bromide | Antiseptic | Topical | 5 |
|
Triple dye (Brilliant green
FW 482.64, Gentian violate FW 408, Proflavine hemisulfate FW 258.29) |
Antiseptic | Topical | 5 |
| Pentamide | Antiprotozoal | Intravenous | >5uM |
| Aurothioglucose | Antirheumatic | Intravenous | >5uM |
| Brilliant Blue | Antiseptic | Topical | >5uM |
| Demecarium bromide | Cholinergic | Topical (ophthalmic) |
>5uM |
| Gold sodium thiomalate | Antirheumatic | Intravenous | >5uM |
| Oxiconazole nitrate | Antifungal | Topical | >5uM |
| Sodium aurothiomalate | Antirheumatic | Intravenous | >5uM |