Synthesis and antibacterial activity of novel benzodioxin-containing oxazolidinones against M. abscessus

IF 2.2 4区 医学 Q3 CHEMISTRY, MEDICINAL
Connor M. Winkelhake , Binayak Rimal , Ben A. Thomas , Joe B. Huisken , Gyanu Lamichhane , J. Thomas Ippoliti
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引用次数: 0

Abstract

Mycobacterium abscessus infections represent a significant treatment challenge, owing to the lack of effective therapies, and the intensive multidrug regimens currently recommended for this indication. Oxazolidinone antibiotics such as linezolid have been used to treat this complex disease. Utilizing a strategic structural extension strategy, five novel oxazolidinone derivatives were synthesized by the introduction of oxime, nitrile, amide, amidoxime, and oxime ester functional groups to a previously reported benzodioxin-scaffold. The in vitro activities of these derivatives against M. abscessus were assessed, with the amidoxime derivative exhibiting activity superior to linezolid.

Abstract Image

新型含苯并二恶唑烷酮类化合物的合成及对脓疡分枝杆菌的抑菌活性研究。
由于缺乏有效的治疗方法,脓肿分枝杆菌感染是一个重大的治疗挑战,目前推荐针对这一适应症的强化多药方案。恶唑烷类抗生素如利奈唑胺已被用于治疗这种复杂的疾病。利用战略性结构扩展策略,将肟、腈、酰胺、偕胺肟和肟酯等官能团引入到先前报道的苯并二氮杂辛支架上,合成了5个新的恶唑烷酮衍生物。这些衍生物对脓肿分枝杆菌的体外活性进行了评估,偕胺肟衍生物的活性优于利奈唑胺。
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来源期刊
CiteScore
5.70
自引率
3.70%
发文量
463
审稿时长
27 days
期刊介绍: Bioorganic & Medicinal Chemistry Letters presents preliminary experimental or theoretical research results of outstanding significance and timeliness on all aspects of science at the interface of chemistry and biology and on major advances in drug design and development. The journal publishes articles in the form of communications reporting experimental or theoretical results of special interest, and strives to provide maximum dissemination to a large, international audience.
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