Novel 4-methoxynaphthalene-N-acylhydrazones as potential for paracoccidioidomycosis and tuberculosis co-infection.

IF 2.4 4区生物学 Q3 MICROBIOLOGY Future microbiology Pub Date : 2019-05-01 Epub Date: 2019-05-31 DOI:10.2217/fmb-2018-0357

Andrew Mf Rozada, Franciele Av Rodrigues, Eloísa G Sampiron, Flavio Av Seixas, Ernani A Basso, Regiane Bl Scodro, Érika S Kioshima, Gisele F Gauze

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引用次数: 13

Abstract

Aim: 17 new 4-methoxynaphthalene-N-acylhydrazones were synthesized in order to evaluate their biological action against important pathogens. Methods: In vitro susceptibility assays of compounds were performed against Paracoccidioidesbrasiliensis and Mycobacterium tuberculosis. Results: Compounds 4a, 4b and 4k were the most potent against P. brasiliensis, two with minimum inhibitory concentrations of ≤1 μg ml^-1 and exhibited pharmacological synergy with amphotericin B. The compounds also showed activity against M. tuberculosis, with 4c and 4k being the more promising. Compound 4k showed good synergistic antimycobacterium activity with ethambutol. None of the compounds tested showed toxicity. Conclusion: We highlight the compound 4k, as a potential agent for the treatment of patients co-infected with paracoccidioidomycosis and tuberculosis.

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新的4-甲氧基萘- n -酰基腙作为潜在的副球孢子菌病和结核病合并感染。

目的:合成17个新的4-甲氧基萘- n -酰基腙，评价其对重要病原菌的生物活性。方法:进行化合物对巴西副球虫和结核分枝杆菌的体外药敏试验。结果:化合物4a、4b和4k对巴西芽孢杆菌的抑制作用最强，其中两种化合物的最低抑制浓度≤1 μg ml-1，且与两性霉素b具有协同作用。化合物对结核分枝杆菌也有一定的抑制作用，其中4c和4k的抑菌效果较好。化合物4k与乙胺丁醇具有较好的协同抑菌活性。测试的化合物都没有显示出毒性。结论:我们强调化合物4k是治疗副球孢子菌病合并结核病的潜在药物。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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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.