香豆素和苯并乙酰基衍生物异烟酸和水杨酸腙的合成及其抑菌活性[j][1,3,5]恶二唑嗪

D.M. Turgunalieva, D.s. Dilbaryan, A. Vasilchenko, O. Nurkenov, S. Fazylov, G. Karipova, Т. Seilkhanov, I. Kulakov
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引用次数: 0

摘要

近几十年来,有机化学、物理和药理学领域的许多研究人员都致力于寻找具有明显抗菌活性,特别是抗真菌活性的新药。这是由于许多细菌菌株和真菌对医疗实践中可用的抗生素和抗真菌药物的耐药性普遍增加。在这方面,科学文献中与从最多样化的有机衍生物合成新的潜在抗生素相关的工作数量正在增加,这些有机衍生物要么包含已知的药效团,要么代表具有未知和未探索活性的新结构类化合物。在这项工作中,在生理活性异烟酸和水杨酸氢氧化物和实验室可用的乙酰取代杂环的基础上,获得了新的先前未描述的腙衍生物,即3-乙酰基- 2h -2- 1 - 3,2 -乙酰基- 3h -苯并[f] -3- 1 - 4和2,6-甲烷苯并[g][1,3,5]恶二唑辛5。所得腙的结构经IR和1H、13C核磁共振谱数据证实。对合成的6个新酰胺对革兰氏阳性菌金黄色葡萄球菌209P、革兰氏阴性菌carotovorum Pectobacterium VKM-B1247和酵母样真菌白色念珠菌ATCC 10231的抑菌活性进行了生物筛选。筛选得到3个具有抗菌活性的化合物和1个有前景的化合物(E)-2-羟基- n ' -(1-(2-氧-3-基)乙基)苯并肼9,该化合物在抗菌活性的同时也具有抗真菌活性。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Synthesis and Antibacterial Activity of Hydrazones of Isonicotinic and Salicylic Acids Based on Acetyl Derivatives of Coumarin and Benzo[g][1,3,5]Oxadiazocine
In recent decades, the efforts of many researchers in the sphere of organic chemistry, physics and pharmacol-ogy have been focused on the search for new agents with pronounced antibacterial and especially antifungal activity. This is due to the widespread increase in the resistance of many bacterial strains and fungi to antibi-otics and antifungal drugs available in medical practice. In this regard, the number of works related to the synthesis of new potential antibiotics from the most diverse class of organic derivatives, which either include known pharmacophore groups or represent a new structural class of compounds with unknown and unex-plored activity, is increasing in the scientific literature. In this work, new previously undescribed hydrazones derivatives were obtained on the basis of physiologically active isonicotinic and salicylic acid hydroxides and laboratory-available acetyl-substituted heterocycles, namely 3-acetyl-2H-chromen-2-one 3, 2-acetyl-3H-benzo[f]chromen-3-one 4 and 2,6-methanobenzo[g][1,3,5]oxadiazocine 5. The obtained hydrazones structure is explicitly proved by IR and 1H, 13C NMR spectroscopy data. The synthesized six new hydrazones under-went biological screening for antibacterial and antifungal activity on strains of microorganisms, namely gram-positive bacterium Staphylococcus aureus 209P, gram-negative bacterium Pectobacterium carotovorum VKM-B1247, and yeast-like fungus Candida albicans ATCC 10231. Screening revealed three compounds with antimicrobial activity and one promising compound — (E)-2-hydroxy-N’-(1-(2-oxochroman-3-yl)ethylidene)benzohydrazide 9, which also exhibits antifungal activity along with antimicrobial activity.
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