一种具有抗分枝杆菌活性的新型 N-酰腙噁二唑衍生物。

IF 2.5 4区生物学 Q3 MICROBIOLOGY

Future microbiology Pub Date : 2024-10-23 DOI:10.1080/17460913.2024.2412439

Izabella Ventura Souza, Maria Luiza Fróes da Motta Dacome, Andrew Matheus Frederico Rozada, Jonathan Sanches Rosa, Eloisa Gibin Sampiron, Deisiany Gomes Ferreira, Gisele Freitas Gauze, Melyssa Fernanda Norman Negri, Regiane Bertin de Lima Scodro, Rosilene Fressatti Cardoso, Katiany Rizzieri Caleffi-Ferracioli

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引用次数: 0

摘要

目的：评估由 N-酰腙（4k）衍生的杂交噁二唑-4-甲氧基萘（6n）的抗结核杆菌（Mtb）潜力：研究确定了 (6n) 对 Mtb H37Rv 和 Mtb 临床分离株的最小抑制浓度、(6n) 与抗结核药物的潜在组合，并对 Mtb H37Rv 进行了时间杀伤曲线测定。通过硅药代动力学、体外和体内细胞毒性测定，对 (6n) 的分析做出了更多贡献：结果：新合成的分子（6n）具有抗 Mtb 活性、低细胞毒性和对 Mtb 的选择性：结论：衍生物（6n）是一种潜在的抗结核候选药物。

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A new N-acylhydrazone oxadiazole derivative with activity against mycobacteria.

Aim: To evaluate the anti-Mycobacterium tuberculosis (Mtb) potential of the hybrid oxadiazol-4-methoxynaphthalene (6n) derived from N-acylhydrazone (4k).Materials & methods: The study determined the minimal inhibitory concentration of (6n) against Mtb H₃₇Rv and Mtb clinical isolates, potential combination of (6n) with anti-tuberculosis drugs and carried out time kill curve assay of Mtb H₃₇Rv. Additional contribution for the analysis of (6n) was explored by in silico pharmacokinetics, and in vitro and in vivo cytotoxicity determinations.Results: The newly synthesized molecule (6n) demonstrated anti-Mtb activity, low cytotoxicity and selectivity for Mtb.Conclusion: The derivative (6n) emerges as a potential anti-TB drug candidate.

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来源期刊

Future microbiology 生物-微生物学

CiteScore

4.90

自引率

3.20%

发文量

134

审稿时长

6-12 weeks

期刊介绍： Future Microbiology delivers essential information in concise, at-a-glance article formats. Key advances in the field are reported and analyzed by international experts, providing an authoritative but accessible forum for this increasingly important and vast area of research.