新型苯并咪唑嵌入的1,3,5-三取代吡唑啉类抗菌剂的合成与表征
Synthesis and characterization of novel benzimidazole embedded 1,3,5-trisubstituted pyrazolines as antimicrobial agents
摘要:
采用多步反应序列,高效合成了一些新型取代吡唑啉衍生物和取代苯并咪唑骨架。所有合成的化合物,其特征在于使用元素分析和光谱研究(IR,1D/2D NMR技术和质谱)。对所合成的化合物进行了抗革兰氏阳性菌、革兰氏阴性菌和真菌的活性筛选。在1-苯基吡唑啉环C5位有卤代苯基取代的化合物(15,16和17)显示出明显的抗菌活性。在筛选的化合物中,17个显示出对细菌菌株的最强抑制活性(MIC = 64 μg mL-1)。供试化合物对真菌C.白色念珠菌,除了吡唑啉-1-硫代羰胺21,其是中度活性的。
英文摘要:
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.
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