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Synthesis and Anti-mycobacterium Study of halo-substituted 2-aryloxyacetohydrazones.
Current Computer-Aided Drug Design ( IF 1.7 ) Pub Date : 2020-09-30 , DOI: 10.2174/1573409915666191018120611
Vijay J Desale 1, 2 , Suraj N Mali 3 , Hemchandra K Chaudhari 3 , Maya C Mali 3 , Bapu R Thorat 2 , Ramesh S Yamgar 4
Affiliation  

Background: The treatment of multiple-drug-resistant tuberculosis (MDR-TB) with currently available marketed drugs remains a global health concern. The cases of resistant tuberculosis patients are increasing day by day.

Objective: The objective of this study is to highlight the need of developing shorter, simpler and tolerable drug regimens.

Methods: In the present study, we synthesized various halo-substituted 2-aryloxyacetohydrazones via a series of reactions from halo-substituted phenols. All the compounds were characterized by using various spectroscopic methods, such as NMR, FT-IR, UV spectroscopy, etc.

Results: All the synthesized hydrazones showed theoretically good interactions with enzyme enoyl reductase (pdb id: 4tzk). All the synthesized compounds (5a-5o) showed moderate to good activity (3.125-100 μg/mL) against Mycobacteria tuberculosis, H37RV strain.

Conclusion: Our results would pave a new way for the development of more effective Anti-TB agents in the future.



中文翻译:

卤代2-芳氧基乙酰腙的合成和抗分枝杆菌研究。

背景:用目前可用的市售药物治疗耐多药结核病 (MDR-TB) 仍然是一个全球性的健康问题。耐药结核病患者的病例日益增多。

目的:本研究的目的是强调开发更短、更简单和可耐受的药物治疗方案的必要性。

方法:在本研究中,我们通过卤代苯酚的一系列反应合成了各种卤代 2-芳氧基乙酰腙。所有化合物均采用核磁共振、傅里叶变换红外光谱、紫外光谱等多种光谱方法进行表征。

结果:所有合成的腙在理论上都显示出与酶烯酰还原酶(pdb id:4tzk)良好的相互作用。所有合成的化合物 (5a-5o) 对结核分枝杆菌 H37RV 菌株均表现出中等至良好的活性 (3.125-100 μg/mL)。

结论:我们的研究结果将为未来开发更有效的抗结核药物铺平道路。

更新日期:2020-11-09
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