Ganfeborole

Last updated

Ganfeborole
Ganfeborole structure.png
Identifiers
  • 2-[[(3S)-3-(Aminomethyl)-4-chloro-1-hydroxy-3H-2,1-benzoxaborol-7-yl]oxy]ethanol
CAS Number
PubChem CID
ChemSpider
UNII
ChEMBL
Chemical and physical data
Formula C10H13BClNO4
Molar mass 257.48 g·mol−1
3D model (JSmol)
  • 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
  • InChI=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
  • Key: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]

References

  1. ↑ Li X, Hernandez V, Rock FL, Choi W, Mak YS, Mohan M, et al. (October 2017). "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. doi:10.1021/acs.jmedchem.7b00631. PMID   28953378.
  2. ↑ Igarashi M, Ishizaki Y, Takahashi Y (November 2017). "New antituberculous drugs derived from natural products: current perspectives and issues in antituberculous drug development". The Journal of Antibiotics. 71: 15–25. doi: 10.1038/ja.2017.126 . PMID   29089593.
  3. ↑ Diacon AH, Barry CE, Carlton A, Chen RY, Davies M, de Jager V, et al. (March 2024). "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. doi:10.1038/s41591-024-02829-7. PMC   10957473 . PMID   38365949.
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