NOVEL β-LACTAMS AND THIAZOLIDINONE DERIVATIVES FROM 1,4-DIHYDROQUINOXALINE SCHIFF'S BASE: SYNTHESIS, ANTIMICROBIAL ACTIVITY AND MOLECULAR DOCKING STUDIES

被引:14
作者
Hrichi, Hajer [1 ,3 ]
Elkanzi, Nadia Ali Ahmed [1 ,2 ]
Bakr, Rania Badawy [4 ,5 ]
机构
[1] Jouf Univ, Coll Sci, Chem Dept, Sakaka 2014, Saudi Arabia
[2] Aswan Univ, Fac Sci, Chem Dept, Aswan 81528, Egypt
[3] Carthage Univ, Natl Inst Appl Sci & Technol, Ctr Urbain Nord, Tunis 1080, Tunisia
[4] Jouf Univ, Dept Pharmaceut Chem, Coll Pharm, Sakaka 2014, Aljouf, Saudi Arabia
[5] Beni Suef Univ, Fac Pharm, Dept Pharmaceut Organ Chem, Bani Suwayf 62514, Egypt
来源
CHEMISTRY JOURNAL OF MOLDOVA | 2020年 / 15卷 / 01期
关键词
heterocycle; beta-lactam; quinoxaline; antimicrobial activity; molecular docking; BIOLOGICAL EVALUATION; QUINOXALINE DERIVATIVES; ANTIOXIDANT; ANTICANCER; RESISTANCE; BINDING; DESIGN;
D O I
10.19261/cjm.2019.647
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
A series of novel isolated beta-lactams 3a-c and thiazolidinone derivatives 4a-c were successfully synthesized from reactions of new Schiff's bases 2a-c with chloroacetyl chloride and thioglycolic acid. The chemical structures of the new compounds were confirmed through different spectroscopic techniques including IR, H-1 and C-13 NMR, mass spectrometry and elemental analysis. The antimicrobial activity of the obtained compounds was assessed in vitro against gram-positive Staphylococcus aureus and gram-negative Escherichia coli bacteria and Aspergillus flavus and Candida albicans fungi. All compounds exhibited good to excellent antimicrobial activity against the tested strains. Furthermore, a molecular docking study was carried out for the synthesized compounds and the results indicated that compounds 3b and 4b display comparable binding affinity scores as that of glutamate. These two compounds are promising candidates as antibacterial and antifungal agents that would deserve further investigations.
引用
收藏
页码:86 / 94
页数:9
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