Synonyms: GSK3036656 | GSK656
Compound class:
Synthetic organic
Comment: Ganfeborole (GSK3036656) is a first-in-class boron-containing antitubercular agent. It is the lead from a series of 3-aminomethylbenzoxaboroles that are potent inhibitors of Mycobacterium tuberculosis leucyl-tRNA synthetase (LeuRS) [2]. We show the (S) enantiomer, which is the most active form.
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References |
1. Dong W, Li S, Wen S, Jing W, Shi J, Ma Y, Huo F, Gao F, Pang Y, Lu J. (2020)
In Vitro Susceptibility Testing of GSK656 against Mycobacterium Species. Antimicrob Agents Chemother, 64 (2). [PMID:31791947] |
2. Li X, Hernandez V, Rock FL, Choi W, Mak YSL, Mohan M, Mao W, Zhou Y, Easom EE, Plattner JJ et al.. (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). J Med Chem, 60 (19): 8011-8026. [PMID:28953378] |
3. Tenero D, Derimanov G, Carlton A, Tonkyn J, Davies M, Cozens S, Gresham S, Gaudion A, Puri A, Muliaditan M et al.. (2019)
First-Time-in-Human Study and Prediction of Early Bactericidal Activity for GSK3036656, a Potent Leucyl-tRNA Synthetase Inhibitor for Tuberculosis Treatment. Antimicrob Agents Chemother, 63 (8). [PMID:31182528] |