Department of Pharmaceutical chemistry, Faculty of Pharmacy, The Islamia University of Bahawalpur, Bahawalpur, 63100, Pakistan.
Institute of Pharmaceutical Science, Faculty of Life Science & Medicine, King's College, London, SE1 9NH, UK.
Future Med Chem. 2023 Dec;15(23):2181-2194. doi: 10.4155/fmc-2023-0225. Epub 2023 Nov 24.
DNA gyrase and urease enzymes are important targets for the treatment of gastroenteritis, appendicitis, tuberculosis, urinary tract infections and Crohn's disease. Esterification of norfloxacin was performed to enhance DNA gyrase and urease enzyme inhibition potential. Structure elucidation and chemical characterization were done through spectral (H NMR, Fourier transform IR, C NMR) and carbon, hydrogen, nitrogen and sulfur analysis along with molecular docking. The majority of derivatives exhibited significant results but the derivative showed maximum bactericidal, DPPH scavenging (96%), DNA gyrase and urease enzyme inhibitory activity with IC of 0.15 ± 0.24 and 1.14 ± 0.11 μM 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.
DNA 回旋酶和脲酶是治疗肠胃炎、阑尾炎、肺结核、尿路感染和克罗恩病的重要靶点。对诺氟沙星进行酯化以增强 DNA 回旋酶和脲酶抑制潜力。通过光谱（H NMR、傅里叶变换红外、C NMR）和碳、氢、氮和硫分析以及分子对接进行结构阐明和化学表征。大多数衍生物表现出显著的结果，但该衍生物表现出最大的杀菌作用、DPPH 清除（96%）、DNA 回旋酶和脲酶抑制活性，IC 分别为 0.15±0.24 和 1.14±0.11 μM，这进一步得到了分子对接研究的支持。因此，这些活性衍生物可以作为治疗各种病理状况的先导化合物。
