Synthesis of 2-hydroxybenzohydrazide derivatives with microwave irradiation and activity against Escherichia coli

IF 0.5 Q4 EDUCATION, SCIENTIFIC DISCIPLINES

Pharmacy Education Pub Date : 2023-10-10 DOI:10.46542/pe.2023.234.279283

None Suzana, None Fika Amalia Najati, None Isnaeni, None Tutuk Budiati

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引用次数: 0

Abstract

Background: This study synthesised derivatives of 2-hydroxybenzohydrazide using microwave irradiation (green chemistry) and tested their antibacterial activity against Escherichia coli. Objective: The reaction yielded N'-Benzylidene-2-hydroxybenzohydrazide, N'-(2-Methoxybenzylidene)-2-hydroxybenzohydrazide, and N'-(4-Methoxybenzylidene)-2-hydroxybenzohydrazide compounds. Prior to compound synthesis, docking was performed with the ENR inhibitor receptor (Pdb.1C14), to determine the antibacterial activity test. Method: The synthesis was carried out using a condensation reaction. Identification of compounds was carried out by UV-VIS, FTIR, and 1H-NMR spectroscopies. Antibacterial activity against E. coli was evaluated using the well method. Molecule docking study was performed using Mollegro virtual docker. Results: The percentage yield of the synthesis of 2-hydroxybenzohydrazide derivatives was obtained at 68-81%. Docking with the ENR inhibitor receptor for these compounds resulted in a lower rerank score than the initial compound (methyl salicylate). These compounds exhibited antibacterial activity against E. coli. Conclusion: These compounds can synthesised using microwave irradiation. N'-(4-methoxybenzylidene)-2-hydroxybenzohydrazide has greater activity against E. coli.

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微波辐照合成2-羟基苯并肼衍生物及其抗大肠杆菌活性研究

背景:本研究利用微波辐照(绿色化学)合成了2-羟基苯并肼衍生物，并测定了其对大肠杆菌的抗菌活性。目的:合成N'-苄基-2-羟基苯并肼、N'-(2-甲氧基苄基)-2-羟基苯并肼和N'-(4-甲氧基苄基)-2-羟基苯并肼化合物。在化合物合成之前，与ENR抑制剂受体(Pdb.1C14)对接，进行抗菌活性测试。方法:采用缩合反应合成。通过紫外可见光谱、红外光谱和核磁共振光谱对化合物进行了鉴定。采用孔法测定其对大肠杆菌的抑菌活性。利用Mollegro虚拟码头进行分子对接研究。结果:2-羟基苯并肼衍生物的合成收率为68 ~ 81%。与这些化合物的ENR抑制剂受体对接导致的重排序评分低于初始化合物(水杨酸甲酯)。这些化合物对大肠杆菌具有抗菌活性。结论:这些化合物可通过微波辐照合成。N′-(4-甲氧基苄基)-2-羟基苯并肼对大肠杆菌具有较强的抗大肠杆菌活性。

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来源期刊

Pharmacy Education EDUCATION, SCIENTIFIC DISCIPLINES-

CiteScore

0.80

自引率

20.00%

发文量

174

期刊介绍： Pharmacy Education journal provides a research, development and evaluation forum for communication between academic teachers, researchers and practitioners in professional and pharmacy education, with an emphasis on new and established teaching and learning methods, new curriculum and syllabus directions, educational outcomes, guidance on structuring courses and assessing achievement, and workforce development. It is a peer-reviewed online open access platform for the dissemination of new ideas in professional pharmacy education and workforce development. Pharmacy Education supports Open Access (OA): free, unrestricted online access to research outputs. Readers are able to access the Journal and individual published articles for free - there are no subscription fees or ''pay per view'' charges. Authors wishing to publish their work in Pharmacy Education do so without incurring any financial costs.