Table 1.
Compounds described in this review.
| Coumpound | Suspected Target | Target Class | Pubmed CID | Reported Minimal Inhibitory Concentration MIC (µM) * author generated data |
Efficasacy demonstrated in an animal model results can be limited by adm routes/ poor Pk/animal models |
Discovery | TB patients |
|---|---|---|---|---|---|---|---|
| Isoniazed | InhA | Cell wall | 3767 | 0.3* | Yes | 1912 | 1952 |
| Rifampicin | RNA polymerase | Transcription | 135398735 | 0.09 | Yes | 1957 | 1971 |
| Meropenem | L,D-transpeptidase | Cell wall | 441130 | 6.5 | Yes | 1976 | 2016 |
| Sanfetrinem | L,D-transpeptidase | Cell wall | 71452 | 5.3 | Yes | 1976? | 2022 Phase 2, NCT05388448 |
| Spectinomycin | 30S subunit of the bacterial ribosome | Protein synthesis inhibitor | 15541 | 150 | low/no activity | 1961 | |
| Spectinamides 1599 | 30S subunit of the bacterial ribosome | Protein synthesis inhibitor | 60173108 | 3.3 | Yes | 2014 | |
| Clarithromycin | 23S rRNA | Protein synthesis inhibitor | 84029 | 8* | No | 1980 | |
| SEQ9 | 23S rRNA | Protein synthesis inhibitor | 0.7 | Yes | 2015 | ||
| Desotamide | 181446 | NA | 1997 | ||||
| Wollamides B | Unknown | 102341742 | 3 | 2014 | |||
| Viomycin | 23S/16S | Translation | 135398671 | 5.8-12 | 1950 | ||
| Capreomycin | 23S/16S | Translation | 3000502 | 5.8-12 | Yes | 1960 | 1966 |
| Histogranine | Unknown/ATP | 16131189 | 6.9 | 1993 | |||
| Amiclenomycin | Biotin pathway | Metabolism | 99594 | 16 | 1975 | ||
| Pyridomycin | InhA | Cell wall | 3037036 | 0.55-3.0 | 1953 | ||
| CPZEN-45 | MraY/murX | Cell wall | 674119859 | 2.3 | Yes | 2003 | Pre-Clinical (Non-GLP) |
| FNDR 20364 | inhibiting ribosome associated Gtpase activity | translation | Unknown | Yes | Unknown | GLP toxicology | |
| Cyclomarin A | ClpC1 | proteostasis | 10772429 | 1999 | |||
| Pleuromutilin | 50S subunit | Translation | 9886081 | 2.2 | Yes | 1951 | |
| Griselimycin | DnaN | Replication inhibitor | 429055 | 0.09 | Yes | 1964 | 1964 |
| Ethionamide | ethA | Cell wall | 2761171 | 4.5* | 1956 | 1965 | |
| Pretomanid | 456199 | 0.3* | 2000 | 2019 | |||
| Kanglemycin A | RNA polymerase | Transcription | 6443924 | 0.36 | Yes | 2018 | |
| Sorangicin A | RNA polymerase | Transcription | 657059 | Unknown | 1985 | ||
| Corallopyronin | RNA polymerase | Transcription | 90477824 | 30 | 1985 | ||
| Fidaxomycin | RNA polymerase | Transcription | 10034073 | 0.24 | 1987 | ||
| PUM | RNA polymerase | Transcription | 72792467 | inactive | 2017 | ||
| D-AAP1 | RNA polymerase | Transcription | 4 | 2017 | |||
| Nargenicin | DnaE1 | Cell wall | 6326334 | 12.5 | 1980 | ||
| Compound 22 (Spiropyrimidinetrione) | DNA Gyrase | Replication inhibitor | 1.7-5.2 | Yes | 2015 | ||
| VXc-486/SPR720 | DNA Gyrase | Replication inhibitor | Yes | 2014 | Phase 2, NCT04553406 | ||
| Compound 17 (Thiazolopyridone ureas) | DNA Gyrase | Replication inhibitor | 2 | Yes | 2014 | ||
| Gepopidacin (GSK2140944) | DNA Gyrase | Replication inhibitor | 25101874 | 0.38 | 2015 |
CID, pubchem compound identification number; DprE1, decaprenylphosphoryl-β-D-ribose 2’-epimerase (Rv3790); EthA, monooxygenase EthA (Rv3854c); DnaN, DNA polymerase III DnaN (Rv0002); ClpC1, TP-dependent Clp protease ATP-binding subunit ClpC (Rv3596c); InhA, NADH-dependent enoyl-[acyl-carrier-protein] reductase (Rv1484); MmpL3, ransmembrane transporter (Rv0206c); LeuRS, leucyl-tRNA synthetase (Rv0041); DnaE1, DNA polymerase III alpha subunit (Rv1547); DHFR, dihydrofolate reductase DfrA (Rv2763c).