Suppr超能文献

2-芳氧基-N-苯基乙酰胺和 N'-(2-芳氧基氧乙酰基)苯甲酰肼衍生物的合成、分子对接和生物评价作为潜在的抗菌剂。

Synthesis, Molecular Docking and Biological Evaluation of 2-Aryloxy-N-Phenylacetamide and N'-(2-Aryloxyoxyacetyl) Benzohydrazide Derivatives as Potential Antibacterial Agents.

机构信息

Department of Pharmaceutical Chemistry, JSS College of Pharmacy, Ooty, 643001, Tamil Nadu, India.

Department of Biotechnology, JSS College of Pharmacy (A Constituent College of JSS Academy of Higher Education and Research), Ooty, 643001, Tamil Nadu, India.

出版信息

Chem Biodivers. 2021 Apr;18(4):e2000907. doi: 10.1002/cbdv.202000907. Epub 2021 Feb 26.

Abstract

A new class of 2-aryloxy-N-phenylacetamide and N'-(2-aryloxyoxyacetyl) benzohydrazide derivatives with different active moieties were synthesized and screened for their antibacterial activity. Structural characterization of synthesized compounds was performed using HR-MS, H-NMR, and C-NMR spectral data. Amongst the synthesized compounds, 4-{2-[2-(2-chloroacetamido)phenoxy]acetamido}-3-nitrobenzoic acid (3h) and 2-chloro-N-(2-{2-[2-(2-chlorobenzoyl)hydrazinyl]-2-oxoethoxy}phenyl)acetamide (3o) have shown good antibacterial activity against a selected panel of bacteria. Besides, compounds also exhibited bactericidal activity against P. aeruginosa (3h, 0.69 μg/mL) and S. aureus (3o, 0.62 μg/mL) as evident by MBC and time-kill kinetics studies. In silico molecular docking and ADMET properties of newly synthesized compounds revealed that compounds could be considered as promising antibacterial agents.

摘要

一类新的 2-芳氧基-N-苯基乙酰胺和 N'-(2-芳氧基氧乙酰)苯甲酰肼衍生物,具有不同的活性部分,被合成并筛选其抗菌活性。合成化合物的结构特征是使用高分辨率质谱、 H-NMR 和 C-NMR 光谱数据进行的。在所合成的化合物中,4-{2-[2-(2-氯乙酰胺基)苯氧基]乙酰胺基}-3-硝基苯甲酸(3h)和 2-氯-N-(2-{2-[2-(2-氯苯甲酰基)肼基]-2-氧代乙氧基}苯基)乙酰胺(3o)表现出对所选一组细菌的良好抗菌活性。此外,化合物还对铜绿假单胞菌(3h,0.69 μg/mL)和金黄色葡萄球菌(3o,0.62 μg/mL)表现出杀菌活性,这可以通过 MBC 和时间杀伤动力学研究证明。新合成化合物的计算机分子对接和 ADMET 性质表明,这些化合物可以被认为是有前途的抗菌剂。

文献检索

告别复杂PubMed语法,用中文像聊天一样搜索,搜遍4000万医学文献。AI智能推荐,让科研检索更轻松。

立即免费搜索

文件翻译

保留排版,准确专业,支持PDF/Word/PPT等文件格式,支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述,25分钟生成高质量综述,智能提取关键信息,辅助科研写作。

立即免费体验