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一些带有1,2,4-三唑部分的新型腙衍生物作为潜在的抗分枝杆菌药物。

Some New Hydrazone Derivatives Bearing the 1,2,4-Triazole Moiety as Potential Antimycobacterial Agents.

作者信息

Özadali Sari Keriman, Ünsal Tan Oya, Sriram Dharmarajan, Balkan Ayla

机构信息

Hacettepe University, Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Ankara, Turkey.

Birla Institute of Technology and Science - Pilani, Pharmacy Group, Medicinal Chemistry and Antimycobacterial Research Laboratory, Hyderabad Campus, Jawahar Nagar, Hyderabad, Andhra Pradesh, India.

出版信息

Turk J Pharm Sci. 2019 Dec;16(4):432-436. doi: 10.4274/tjps.galenos.2018.43660. Epub 2019 Nov 11.

DOI:10.4274/tjps.galenos.2018.43660
PMID:32454746
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7227891/
Abstract

OBJECTIVES

The aim of this study was to synthesize, characterize, and screen some new 1-(4-((2-(4-substitutedphenyl)hydrazono)methyl)phenyl)-1H-1,2,4-triazole derivatives for their antimycobacterial activities.

MATERIALS AND METHODS

The target compounds were gained by condensation of 4-(1-1,2,4-triazol-1-yl)benzaldehyde with appropriate phenylhydrazines. Their structures were elucidated by IR, H-NMR, and mass spectrometry. The antimycobacterial activities of the compounds were determined against H37Rv.

RESULTS

The biological assay results showed that the methylsulfonyl-substituted derivative displayed the highest antimycobacterial activity in this series.

CONCLUSION

Although the methylsulfonyl-substituted derivative exhibited significant antimycobacterial activity, none of the synthesized compounds was as effective as isoniazid, rifampin, ethambutol, and ciprofloxacin against .

摘要

目的

本研究旨在合成、表征并筛选一些新型1-(4-((2-(4-取代苯基)肼基)甲基)苯基)-1H-1,2,4-三唑衍生物的抗分枝杆菌活性。

材料与方法

目标化合物通过4-(1-1,2,4-三唑-1-基)苯甲醛与适当的苯肼缩合得到。通过红外光谱、氢核磁共振谱和质谱对其结构进行了阐明。测定了这些化合物对H37Rv的抗分枝杆菌活性。

结果

生物学测定结果表明，甲基磺酰基取代的衍生物在该系列中表现出最高的抗分枝杆菌活性。

结论

尽管甲基磺酰基取代的衍生物表现出显著的抗分枝杆菌活性，但所合成的化合物中没有一种在抗[此处原文缺失具体对象]方面像异烟肼、利福平、乙胺丁醇和环丙沙星那样有效。