新型苯并咪唑包埋1,3,5-三取代吡唑啉抗菌药物的合成与表征

Gopal Krishna Padhy, J. Panda, A. Behera
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引用次数: 6

摘要

以取代苯并咪唑为骨架,采用多步反应序列高效合成了几种新型取代吡唑啉衍生物。所有合成的化合物都通过元素分析和光谱研究(IR, 1D/2D NMR技术和质谱)进行了表征。合成的化合物对选定的革兰氏阳性菌、革兰氏阴性菌和真菌的抑菌活性进行了筛选。在1-苯基吡唑啉环(15、16和17)C5位置有环取代苯基的化合物具有明显的抗菌活性。在筛选的化合物中,17种化合物对菌株的抑制活性最强(MIC = 64 {\mu}g mL-1)。实验发现,除了吡唑啉-1-碳硫胺21具有中等活性外,这些化合物对真菌菌株白色念珠菌几乎没有活性。
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Synthesis and characterization of novel benzimidazole embedded 1,3,5-trisubstituted pyrazolines as antimicrobial agents
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 {\mu}g 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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