Synthesis, antimicrobial and molecular docking study of structural analogues of 3-((5-(dimethylcarbamoyl)pyrrolidin-3-yl)thio)-6-(1-hydroxyethyl)-4-methyl-7-oxo-1-azabicyclo[3.2.0]heptane-2-carboxylic acid

被引:2
作者
Khaliq, Saharish [1 ]
Khan, Mohsin Abbas [1 ]
Ahmad, Irshad [1 ]
Ahmad, Imtiaz [1 ,2 ]
Ahmed, Javed [1 ]
Ullah, Farhat [1 ]
机构
[1] Islamia Univ Bahawalpur, Fac Pharm, Dept Pharmaceut Chem, Bahawalpur, Pakistan
[2] Univ Minnesota, Coll Pharm, Dept Med Chem, Minneapolis, MN 55455 USA
来源
PLOS ONE | 2022年 / 17卷 / 12期
关键词
ANTIBACTERIAL ACTIVITY; BETA-LACTAMS; MEROPENEM; ANTIOXIDANT; INHIBITORS; DRUGS;
D O I
10.1371/journal.pone.0278684
中图分类号
O [数理科学和化学]; P [天文学、地球科学]; Q [生物科学]; N [自然科学总论];
学科分类号
07 ; 0710 ; 09 ;
摘要
The goal of the current work was to create structural analogues of a beta lactam antibiotic that might be possibly effective against bacterial resistant strains. FTIR, H-1 NMR, C-13 NMR, and CHNS analyses were used to perform the spectroscopic study on the compounds M1-8. The effects of the aforementioned substances on gram-positive and gram-negative bacterial strains were investigated. Most of the eight compounds had antibacterial activity that was lower than or equivalent to that of the original medication, but two molecules, M-2 and M-3, surprisingly, had stronger antibacterial activity. The findings of synthesized analogues against alpha-glucosidase and DPPH inhibition were found to be modest, whereas M-2, M-3, and M-7 strongly inhibited the urease. To comprehend the potential mode of action, a molecular docking research was conducted against urease and -amylase. The research may help in the quest for novel chemical compounds that would be effective against bacteria that are resistant to antibiotics.
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页数:14
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