TB Discovery Research, Infectious Disease Research Institute, Seattle, Washington, USA.
Anacor Pharmaceuticals, Palo Alto, California, USA.
Antimicrob Agents Chemother. 2017 Aug 24;61(9). doi: 10.1128/AAC.01205-17. Print 2017 Sep.
We identified a novel 6-benzyl ether benzoxaborole with potent activity against The compound had an MIC of 2 μM in liquid medium. The compound was also able to prevent growth on solid medium at 0.8 μM and was active against intracellular bacteria (50% inhibitory concentration [IC] = 3.6 μM) without cytotoxicity against eukaryotic cells (IC > 100 μM). We isolated resistant mutants (MIC ≥ 100 μM), which had mutations in Rv1683, Rv3068c, and Rv0047c.
我们发现了一种新型的 6-苄醚苯并硼唑，对具有很强的活性。该化合物在液体培养基中的 MIC 为 2 μM。该化合物还能够以 0.8 μM 的浓度防止在固体培养基中生长，并且对细胞内细菌有效（50%抑制浓度[IC] = 3.6 μM），而对真核细胞无细胞毒性（IC>100 μM）。我们分离了耐药突变体（MIC≥100 μM），它们在 Rv1683、Rv3068c 和 Rv0047c 中发生了突变。
