首页> 外文期刊>Journal of enzyme inhibition and medicinal chemistry. >Synthesis, antimicrobial and antimycobacterial evaluation of (2-(substituted phenyl)-imidazol-1-yl)-pyridin-3-yl-methanones.
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Synthesis, antimicrobial and antimycobacterial evaluation of (2-(substituted phenyl)-imidazol-1-yl)-pyridin-3-yl-methanones.

机译:(2-(取代的苯基)-咪唑-1-基)-吡啶-3-基-甲烷的合成,抗菌和抗分枝杆菌评估。

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摘要

A series of [2-(substituted phenyl)-imidazol-1-yl]-pyridin-3-yl-methanones (1-11) were synthesized and screened for their antimicrobial and antimycobacterial activities. Further, a series of [2-(substituted phenyl)-benzimidazol-1-yl]-pyridin-3-yl-methanones (12-20) reported in our earlier study was also screened for their antimycobacterial activity. The antimycobacterial activity results indicated that [2-(4-Nitro-phenyl)-imidazol-1-yl]-pyridin-3-yl-methanone (8, minimum inhibitory concentration [MIC] = 3.13 microg) was equipotent as standard drug ciprofloxacin and [2-(4-Nitro-phenyl)-benzimidazol-1-yl]-pyridin-3-yl-methanone (16, MIC = 1.56 microg) was equipotent as standard drug ethambutol. The results of antimicrobial screening demonstrated that 2-[1-(Pyridine-3-carbonyl)-1H-imidazol-2-yl]-benzoic acid (compound 11, MIC = 0.002 microg) was two times more effective than standard drug ciprofloxacin (MIC = 0.004 microg) against tested bacterial strains and [2-(2,5-Dimethyl-phenyl)-imidazol-1-yl]-pyridin-3-yl-methanone (compound 3, MIC = 0.005 microg) was equipotent to the reference compound, fluconazole against tested fungal strains.
机译:合成了一系列的[2-(取代的苯基)-咪唑-1-基]-吡啶-3-基-甲酮(1-11),并筛选了它们的抗微生物和抗分枝杆菌活性。此外,还筛选了我们较早研究中报道的一系列[2-(取代苯基)-苯并咪唑-1-基]-吡啶-3-基-甲酮(12-20)的抗分枝杆菌活性。抗分枝杆菌活性结果表明,[2-(4-硝基-苯基)-咪唑-1-基]-吡啶-3-基-甲酮(8,最低抑菌浓度[MIC] = 3.13 microg)与标准环丙沙星等效[2-(4-硝基-苯基)-苯并咪唑-1-基]-吡啶-3-基-甲酮(16,MIC = 1.56 microg)等价用作标准药物乙胺丁醇。抗菌筛选结果表明,2- [1-(吡啶-3-羰基)-1H-咪唑-2-基]-苯甲酸(化合物11,MIC = 0.002微克)比标准药物环丙沙星( MIC = 0.004 microg)对测试的细菌菌株和[2-(2,5-二甲基-苯基)-咪唑-1-基]-吡啶-3-基-甲酮(化合物3,MIC = 0.005 microg)等价于参比化合物氟康唑抗真菌菌株。

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