论文标题
新型苯唑唑嵌入1,3,5三转化的吡唑啉作为抗菌剂的合成和表征
Synthesis and characterization of novel benzimidazole embedded 1,3,5-trisubstituted pyrazolines as antimicrobial agents
论文作者
论文摘要
通过多步反应序列进行了一些与取代的苯并咪唑支架相关的新替代吡唑啉衍生物的有效合成。使用元素分析和光谱研究(IR,1D/2D NMR技术和质谱法)对所有合成化合物进行表征。对合成化合物的抗菌活性进行了筛选,以针对选定的革兰氏阳性和革兰氏阴性细菌和真菌菌株进行抗菌活性。 1-苯基吡唑啉环(15、16和17)的C5处的光环取代苯基的化合物显示出明显的抗菌活性。在筛选的化合物中,17个对细菌菌株的最有效抑制活性(MIC =64μgml-1)。除了吡唑啉-1-核苷21外,经过测试的化合物几乎是对真菌菌株白色念珠菌几乎没有活性的,该甲基胺1-甲基胺21(中等活性)。
Efficient syntheses of some new substituted pyrazoline derivatives linked to substituted benzimidazole scaffold were performed by multistep reaction sequences. All the synthesized compounds were characterized using elemental analysis and spectral studies (IR, 1D/2D NMR techniques and mass spectrometry). The synthesized compounds were screened for their antimicrobial activity against selected Gram-positive and Gram-negative bacteria, and fungi strain. The compounds with halo substituted phenyl group at C5 of the 1-phenyl pyrazoline ring (15, 16 and 17) showed significant antibacterial activity. Among the screened compounds, 17 showed most potent inhibitory activity (MIC = 64 μg mL-1) against a bacterial strain. The tested compounds werefound to be almost inactive against the fungal strain C. albicans, apart from pyrazoline-1-carbothiomide 21, which was moderately active.