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In vitro antimicrobial activities of animal-used quinoxaline 1,4-di- N -oxides against mycobacteria, mycoplasma and fungi

机译:动物用喹喔啉1,4-二-N-氧化物对分枝杆菌,支原体和真菌的体外抗菌活性

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Background The quinoxaline 1,4-di- N -oxides (QdNOs) were known as potent antibacterial agents. For the purpose of evaluating the bioactivity of existing animal-used QdNOs drugs against representative pathogenic microorganism, the representative drugs of quinoxalines including cyadox, mequindox, quinocetone and their metabolites were submitted to the in vitro evaluation for antituberculosis, antimycoplasma, antifungal and antiviral activities. Results In antituberculosis assays, the prototype compounds were active (MIC?=?4?~?8?μg/mL) against Mycobacterium tuberculosis H37Rv and M. bovis. Combined antimicrobial susceptibility test indicated that cyadox, mequindox and quinocetone combined with rifampicin had additive effect against M. tuberculosis complex with Fractional Inhibitory Concentration Index (FIC) of 0.75. Results of antifungal assays showed that quinocetone was active against Microsporum canis with MIC of 8?μg/mL. Antimycoplasma screening showed a generally good activity of quinocetone against Mycoplasma gallisepticum and Mycoplasma hyopneumoniae , with MIC between 8 and 16?μg/mL. As shown from the combined antimicrobial susceptibility test, cyadox, mequindox and quinocetone combined with tetracycline had additive effect against Mycoplasma gallisepticum with FIC of 0.75. These compounds were also submitted to antiviral assay against infectious bursal disease virus, porcine reproductive and respiratory syndrome virus, porcine parvovirus and classical swine fever virus. The results obtained showed that these QdNOs and their metabolites have no inhibitory activity against these viruses in vitro. Conclusions QdNOs exhibit antimicrobial activities against mycobacteria, mycoplasma and fungi. This study gives new insight in further application of QdNOs and offers a way to promote the healthcare of animal husbandry.
机译:背景技术喹喔啉1,4-二-N-氧化物(QdNOs)被认为是有效的抗菌剂。为了评估现有的动物用QdNOs药物对代表性致病微生物的生物活性,将喹喔啉的代表性药物(包括cyadox,mequindox,喹诺酮及其代谢产物)进行了体外评估,以评估抗结核,抗支原体,抗真菌和抗病毒活性。结果在抗结核试验中,原型化合物对结核分枝杆菌H37Rv和牛分枝杆菌有活性(MIC≥=4≥〜8?μg/ mL)。联合药敏试验表明,cyadox,mequindox和quinocetone与利福平联合使用对结核分枝杆菌复合物具有累加作用,分数抑制浓度指数(FIC)为0.75。抗真菌试验结果表明喹诺酮对犬小孢子菌有活性,MIC为8?μg/ mL。抗支原体筛选显示喹烯酮对鸡支原体和猪肺炎支原体的总体活性良好,MIC在8至16?g / mL之间。如联合抗菌药敏试验所示,cyadox,mequindox和quinocetone与四环素联合使用对鸡支原体的加和作用,FIC为0.75。这些化合物也已针对传染性法氏囊病病毒,猪生殖和呼吸综合症病毒,猪细小病毒和经典猪瘟病毒进行了抗病毒测定。获得的结果表明,这些QdNOs及其代谢产物在体外对这些病毒没有抑制活性。结论QdNOs对分枝杆菌,支原体和真菌具有抗菌活性。这项研究为进一步应用QdNOs提供了新的见识,并为促进畜牧业的保健提供了一种途径。

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