Ganfeborole Explained
| Drug Name: | Ganfeborole |
| C: | 10 |
| H: | 13 |
| B: | 1 |
| Cl: | 1 |
| N: | 1 |
| O: | 4 |
| Iupac Name: | 2-(3S)-3-(Aminomethyl)-4-chloro-1-hydroxy-3H-2,1-benzoxaborol-7-yloxy]ethanol |
| Cas Number: | 2131798-12-2 |
| Chemspiderid: | 71046056 |
| Pubchem: | 133080621 |
| Unii: | KZ8H57WFC7 |
| Chembl: | 4116378 |
| Smiles: | B1(C2=C(C=CC(=C2[C@H](O1)CN)Cl)OCCO)O(C(=O)N1)CCN)CCN)CC(C)C)CC2=CC=CC=C2)CCN)NC(=O)[C@@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)C)O |
| Stdinchi: | 1S/C10H13BClNO4/c12-6-1-2-7(16-4-3-14)10-9(6)8(5-13)17-11(10)15/h1-2,8,14-15H,3-5,13H2/t8-/m1/s1 |
| Stdinchikey: | DJUOWOXTPXUHDQ-MRVPVSSYSA-N |
Ganfeborole (GSK3036656, GSK-070) is an experimental antibiotic which shows activity against Mycobacterium tuberculosis. It acts as a potent and selective inhibitor of the bacterial leucyl-tRNA synthetase enzyme, and is currently in clinical trials.[1] [2] [3]
Notes and References
- Li X, Hernandez V, Rock FL, Choi W, Mak YS, Mohan M, Mao W, Zhou Y, Easom EE, Plattner JJ, Zou W, Pérez-Herrán E, Giordano I, Mendoza-Losana A, Alemparte C, Rullas J, Angulo-Barturen I, Crouch S, Ortega F, Barros D, Alley MR . Discovery of a Potent and Specific M. tuberculosis Leucyl-tRNA Synthetase Inhibitor: (S)-3-(Aminomethyl)-4-chloro-7-(2-hydroxyethoxy)benzo[c][1,2]oxaborol-1(3H)-ol (GSK656) . Journal of Medicinal Chemistry . 60 . 19 . 8011–8026 . October 2017 . 28953378 . 10.1021/acs.jmedchem.7b00631 .
- Igarashi M, Ishizaki Y, Takahashi Y . New antituberculous drugs derived from natural products: current perspectives and issues in antituberculous drug development . The Journal of Antibiotics . 71. 15–25. November 2017 . 29089593 . 10.1038/ja.2017.126 .
- Diacon AH, Barry CE, Carlton A, Chen RY, Davies M, de Jager V, Fletcher K, Koh GC, Kontsevaya I, Heyckendorf J, Lange C, Reimann M, Penman SL, Scott R, Maher-Edwards G, Tiberi S, Vlasakakis G, Upton CM, Aguirre DB . A first-in-class leucyl-tRNA synthetase inhibitor, ganfeborole, for rifampicin-susceptible tuberculosis: a phase 2a open-label, randomized trial . Nature Medicine . 30 . 3 . 896–904 . March 2024 . 38365949 . 10957473 . 10.1038/s41591-024-02829-7 .
