吲哚基二苯甲酮及其衍生物的设计、合成及抗菌活性评价

Fekadu Tumoro Erabe, D. Kure, S. Sheri̇f
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引用次数: 0

摘要

吲哚和二苯甲酮片段引起了研究人员的极大兴趣,因为它们存在于许多天然产物和具有药理活性的化合物中。它们代表了多功能的合成构件。二苯甲酮和吲哚支架是药物化学中的特殊结构,因为这些化合物存在于几种具有生物活性的天然产物中,含有吲哚和二苯甲酮的化合物具有抗癌、抗炎、抗菌和抗病毒活性。本研究成功合成了含吲哚和二苯甲酮的2-(二苯基亚甲基)肼衍生物。利用IR、1HNMR和13CNMR等光谱技术对合成的化合物进行了结构分析。研究了合成的目标化合物对两种细菌的体外抗菌活性;金黄色葡萄球菌(S. auras)和大肠杆菌(E. coli)采用圆盘扩散法。所有合成的目标化合物对金黄色葡萄球菌(S. aureus)无显著活性,但对大肠杆菌(E. coli)有中等活性。在所合成的化合物中,2-(二苯基亚甲基)-1-((1-甲酰基- 1h -吲哚-3-酰基)亚甲基肼(BHT) (7b)对大肠杆菌(E.coli)有良好的抑制作用,浓度为50 μg/mL,抑制区为21.7 mm,与标准药物头孢曲松相当,抑制区为26 mm。因此,该化合物可作为设计和开发新型抗菌药物的先导分子。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Design, Synthesis and Anti-Bacterial Activity Evaluation of Indole-Based Benzophenone and Their Derivatives
Indole and benzophenone moiety are of significant interest to investigators because they are found in many natural products and pharmacologically active compounds. They represent versatile synthetic building blocks. The benzophenone and indole scaffolds are special structures in medicinal chemistry because these compounds are found in several biologically active natural products, compounds containing indole and benzophenone exhibit anticancer, antiinflammatory, antimicrobial, and antiviral activities. In this study, derivatives of 2-(diphenyl methylene) hydrazine, containing both indole and benzophenone moieties were successfully synthesized. The structural elucidation of the synthesized compounds were done using spectroscopic techniques like IR, 1HNMR, and 13CNMR. The synthesized target compounds were investigated for their in vitro antibacterial activity against two bacterial strains; staphylococcus aureus (S. auras), and Escherichia coli (E. coli) using the disc diffusion method. All synthesized target compounds showed no significant activity against Staphylococcus aureus (S. aureus) but exhibited moderate activity against Escherichia coli (E. coli). Among all the synthesized compounds, 2-(diphenyl methylene)-1-((1-tosyl-1H-indol-3-yl) methylene) hydrazine (BHT) (7b) showed a good inhibition at a concentration of 50 μg/mL with a zone of inhibition of 21.7 mm against Escherichia coli (E.coli) which was comparable with standard drug Ceftriaxone with the zone of inhibition of 26 mm. Thus, this compound could be considered as a lead molecule to design and develop novel antibacterial drugs.
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