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首页> 外文期刊>Bioorganic and Medicinal Chemistry Letters >Identification of novel 2-aminothiazole conjugated nitrofuran as antitubercular and antibacterial agents
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Identification of novel 2-aminothiazole conjugated nitrofuran as antitubercular and antibacterial agents

机译：新型2-氨基噻唑共轭硝基呋喃作为抗结核和抗菌药物的鉴定

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摘要

The emergence of antibiotic resistant pathogens is an ongoing main problem in the therapy of bacterial infections. In order to develop promising antitubercular and antibacterial lead compounds, we designed and synthesized a new series of derivatives of 2-aminothiazole conjugated nitrofuran with activities against both Mycobacterium tuberculosis and Staphylococcus aureus. Eight compounds 12e, 12k, 12l, 12m, 18a, 18d, 18e, and 18j emerged as promising antitubercular agents. Structure-activity relationships (SARs) were discussed and showed that the derivatives substituted at the position-3 of benzene of 5-nitro-N-(4-phenylthiazol-2-yl) furan-2-carboxamide exhibited superior potency. The most potent compound 18e, substituted with benzamide at this position, displayed minimum inhibitory concentrations (MICs) of 0.27 mu g/mL against Mtb H37Ra and 1.36 mu g/mL against S. aureus. Furthermore, compound 18e had no obvious cytotoxicity to normal Vero cells (IC50 = 50.2 mu M). The results suggest that the novel scaffolds of aminothiazole conjugated nitrofuran would be a promising class of potent antitubercular and antimicrobial agents. (C) 2016 Elsevier Ltd. All rights reserved.
机译：抗生素抗性病原体的出现是细菌感染治疗中的主要问题。为了开发有前途的抗结核和抗菌先导化合物，我们设计并合成了一系列新的2-氨基噻唑共轭硝基呋喃衍生物，具有对抗结核分枝杆菌和金黄色葡萄球菌的活性。出现了八种化合物12e，12k，12l，12m，18a，18d，18e和18j作为有希望的抗结核药。讨论了结构-活性关系（SARs），结果表明，在5-硝基-N-（4-苯基噻唑-2-基）呋喃-2-羧酰胺的苯位置3处取代的衍生物表现出优异的效能。最有效的化合物18e在该位置被苯甲酰胺取代，对Mtb H37Ra的最低抑菌浓度（MIC）为0.27μg/ mL，对金黄色葡萄球菌的抑菌浓度为1.36μg/ mL。此外，化合物18e对正常的Vero细胞没有明显的细胞毒性（IC50 = 50.2μM）。结果表明，氨基噻唑共轭硝基呋喃的新型支架将是一类有前景的强效抗结核和抗菌剂。 （C）2016 Elsevier Ltd.保留所有权利。

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