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埃泼拉博雷有效对抗脓肿分枝杆菌。

Epetraborole Is Active against Mycobacterium abscessus.

机构信息

Center for Discovery and Innovation, Hackensack Meridian Health, Nutley, New Jersey, USA.

Department of Medical Sciences, Hackensack Meridian School of Medicine, Nutley, New Jersey, USA.

出版信息

Antimicrob Agents Chemother. 2021 Sep 17;65(10):e0115621. doi: 10.1128/AAC.01156-21. Epub 2021 Jul 19.

Abstract

Benzoxaboroles are a new class of leucyl-tRNA synthetase inhibitors. We recently reported that the antitubercular 4-halogenated benzoxaboroles are active against Mycobacterium abscessus. Here, we find that the nonhalogenated benzoxaborole epetraborole, a clinical candidate developed for Gram-negative infections, is also active against M. abscessus and in a mouse model of infection. This expands the repertoire of advanced lead compounds for the discovery of a benzoxaborole-based candidate to treat M. abscessus lung disease.

摘要

苯并恶唑硼烷是一类新型亮氨酰-tRNA 合成酶抑制剂。我们最近报道称,具有抗结核作用的 4-卤代苯并恶唑硼烷对脓肿分枝杆菌具有活性。在此,我们发现非卤代苯并恶唑硼烷依匹特罗硼烷(一种针对革兰氏阴性感染开发的临床候选药物)也对脓肿分枝杆菌有效,并且在感染的小鼠模型中也有效。这扩大了用于发现基于苯并恶唑硼烷的候选药物以治疗脓肿分枝杆菌肺病的先进先导化合物库。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/661e/8448144/8b2766fa1deb/aac.01156-21-f001.jpg

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