新型苯并咪唑曼尼希碱衍生物的设计、合成、表征和抗结核活性

Q4 Chemistry Asian Journal of Chemistry Pub Date : 2024-03-30 DOI:10.14233/ajchem.2024.31314
C. Gopi, M. Dhanaraju, Konatham Pranusha, Thiyagarajan Deepan, AR Magesh, Dhanaraju Kavitha
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引用次数: 0

摘要

在本研究中,我们设计、合成了新合成的苯并咪唑曼尼希碱衍生物,并对其进行了硅学和体外抗结核活性评估。这些化合物是通过 1-(1H-苯并[d]咪唑-1-基)乙酮和脂肪族/芳香族胺的缩合反应合成的。合成的化合物结构通过傅立叶变换红外光谱、13C NMR、1H NMR 和质谱进行了鉴定。结果表明,这些衍生物对 H73Rv 菌株中的结核分枝杆菌(M.tb)细胞壁酶烯酰酰基载体蛋白还原酶(InhA)和 EthR 调节蛋白具有显著的抗结核活性。体外研究结果与硅学研究结果非常相似。在合成的化合物中,3d 和 3e 的活性最高,这是因为电子供能基团与曼尼希碱的连接。因此,这些化合物值得开发成新的抗结核药物。
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Design, Synthesis, Characterization and Antitubercular Activity of Novel Benzimidazole Mannich Base Derivatives
In present work, the newly synthesized benzimidazole Mannich base derivatives were design, synthesized and evaluated the in silico and in vitro antitubercular activity. These compounds were synthesized by condensation reaction between 1-(1H-benzo[d]imidazol-1-yl)ethanone and aliphatic/aromatic amines. The synthesized compound structures were identified by FTIR, 13C NMR, 1H NMR and mass spectroscopies. The results indicated that these derivatives have significant antitubercular activity against Mycobacterium tuberculosis (M.tb) cell wall enzyme enoyl acyl carrier protein reductase (InhA), EthR regulatory protein in H73Rv strain. The results found in the in vitro study are firmly similar to the in silico study. Among the synthesized compounds, 3d and 3e exhibited the highest activity due to the connection of the electron-donating group to the Mannich base. Therefore, these compounds deserve the development of new antitubercular agents.
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来源期刊
Asian Journal of Chemistry
Asian Journal of Chemistry 化学-化学综合
CiteScore
0.80
自引率
0.00%
发文量
229
审稿时长
4 months
期刊介绍: Information not localized
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