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