Norfloxacin derivatives as DNA gyrase and urease inhibitors: synthesis, biological evaluation and molecular docking

被引：3
|
作者：
Awan, Breena [1 ]
Khan, Mohsin Abbas [1 ,2 ]
Ahmad, Irshad [1 ]
Masood, Anum [1 ]
Raza, Asim [1 ]
Khaliq, Saharish [1 ]
Ullah, Farhat [1 ]
Ahmed, Javed [1 ]
Khan, Muhammad Rizwan [1 ]
机构：
[1] Islamia Univ Bahawalpur, Fac Pharm, Dept Pharmaceut Chem, Bahawalpur 63100, Pakistan
[2] Kings Coll London, Inst Pharmaceut Sci, Fac Life Sci & Med, London SE1 9NH, England
来源：
FUTURE MEDICINAL CHEMISTRY | 2023年 / 15卷 / 23期
关键词：
bactericidal; DPPH scavenging; enzyme inhibition; esters; ACCURATE DOCKING; SCHIFF-BASES; ANTIBACTERIAL; COMPLEXES; GLIDE;
D O I：
10.4155/fmc-2023-0225
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Background: DNA gyrase and urease enzymes are important targets for the treatment of gastroenteritis, appendicitis, tuberculosis, urinary tract infections and Crohn's disease. Materials & methods: Esterification of norfloxacin was performed to enhance DNA gyrase and urease enzyme inhibition potential. Structure elucidation and chemical characterization were done through spectral (1H NMR, Fourier transform IR, C-13 NMR) and carbon, hydrogen, nitrogen and sulfur analysis along with molecular docking. Results & conclusion: The majority of derivatives exhibited significant results but the 3e derivative showed maximum bactericidal, DPPH scavenging (96%), DNA gyrase and urease enzyme inhibitory activity with IC50 of 0.15 +/- 0.24 and 1.14 +/- 0.11 mu M respectively which was further supported by molecular docking studies. So, the active derivatives can serve as a lead compound for the treatment of various pathological conditions. [GRAPHICS] .
引用
收藏
页码：2181 / 2194
页数：14
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