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首页> 外文期刊>The Journal of Antibiotics: An International Journal >Antibacterial, antifungal and antileishmanial activities of indolone-N-oxide derivatives
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Antibacterial, antifungal and antileishmanial activities of indolone-N-oxide derivatives

机译：吲哚酮-N-氧化物衍生物的抗菌，抗真菌和抗菌活性

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摘要

An alarming increase in microbial resistance to traditional drugs and classical pharmacophores has spurred the search for new antimicrobial compounds. Indolone-N-oxides (INODs) possess a redox pharmacophore with promising, recently established, antimalarial activities. In this study, the anti-infectious properties of a series of INODs were investigated. The antibacterial activity was evaluated against five bacterial strains Gram-positive (Staphylococcus aureus, Enterococcus hirae), Gram-negative (Pseudomonas aeruginosa, Escherichia coli) and acid-fast (Mycobacterium tuberculosis). The antifungal activity was assessed using two fungal strains (Aspergillus niger, Candida albicans). The antileishmanial activity was tested against two leishmanial strains, axenically-cultured amastigote (Leishmania infantum, Leishmania amazonensis). The pharmacological activities are discussed as a function of structural and lipophilic characteristics. The Gram-positive bacterial strain E. hirae was found to be the most sensitive strain, whereas the Gram-negative E. coli was resistant to this family of compounds. One compound (64) was more potent than nalidixic acid against E. hirae, whereas another one (52) was equipotent as clotrimazole against C. albicans. INODs were microbe -cidal rather than -static. INODs showed good antitubercular activity in the low micromolar range (similar to ciprofloxacin). In addition, INOD-antiprotozoal potencies were confirmed against the leishmania parasite. INODs showed a broad spectrum of antimicrobial activity and offer a promising anti-infectious prototype worthy of being developed.
机译：微生物对传统药物和经典药效团的耐药性惊人地增加，促使人们寻找新的抗微生物化合物。吲哚酮-N-氧化物（INODs）具有氧化还原药效基团，具有很强的，最近建立的抗疟活性。在这项研究中，研究了一系列INOD的抗感染特性。评估了对五种革兰氏阳性（金黄色葡萄球菌，平肠肠球菌），革兰氏阴性（铜绿假单胞菌，大肠杆菌）和耐酸菌株（耐结核分枝杆菌）的抗菌活性。使用两种真菌菌株（黑曲霉，白色念珠菌）评估抗真菌活性。测试了抗利什曼活性针对两种利什曼菌株，即无菌培养的鞭毛体（Leishmania infantum，Leishmania amazonensis）。讨论了作为结构和亲脂特性的函数的药理活性。发现革兰氏阳性细菌菌株平肠埃希氏菌是最敏感的菌株，而革兰氏阴性大肠杆菌对该化合物家族具有抗性。一种化合物（64）在抗埃希氏大肠杆菌方面比萘啶酸更有效，而另一种化合物（52）在抗白念珠菌方面具有克霉唑的功效。 INODs具有杀微生物作用，而不具有静电作用。 INODs在低微摩尔范围内显示出良好的抗结核活性（类似于环丙沙星）。另外，证实了针对利什曼原虫寄生虫的INOD-抗原生动物效力。 INODs具有广泛的抗菌活性，并提供了值得开发的有希望的抗感染原型。

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