2. Academic Validation
  3. Design, synthesis and biological evaluation of novel fluoroquinolone-uracil hybrids against methicillin-resistant Staphylococcus Epidermidis (MRSE) infections

Design, synthesis and biological evaluation of novel fluoroquinolone-uracil hybrids against methicillin-resistant Staphylococcus Epidermidis (MRSE) infections

  • Bioorg Chem. 2026 Jun 5:173:109657. doi: 10.1016/j.bioorg.2026.109657.
Huan Du 1,  Qiong Yang 2,  Le Li 1,  Long Chen 3,  Hua Liang 1,  Hehuan Sui 4,  Jielu Wei 5,  Pengyue Li 1,  Hui Wang 1,  Yutong Fu 6,  Qisen Yang 1,  Jinyou Duan 7
Affiliations

Affiliations

  • 1 College of Chemistry and Pharmacy, Northwest A&F University, Yangling 712100, Shaanxi, PR China.
  • 2 School of Chinese Ethnic Medicine, Guizhou Minzu University, Guiyang 550025, Guizhou, China.
  • 3 College of Chemical and Materials Engineering, Key Laboratory of Green Processing and Intelligent Manufacturing of Lingnan Specialty Food, Ministry of Agriculture, Zhongkai University of Agriculture and Engineering, Guangzhou 510225, PR China.
  • 4 The First Affiliated Hospital of Chongqing Medical University, 400016 Chongqing, China.
  • 5 School of Pharmacy, Gansu Medical College, 744000 Pingliang, Gansu, China.
  • 6 College of Water Resources and Architectural Engineering, Northwest A&F University, Yangling 712100, Shaanxi, PR China.
  • 7 College of Chemistry and Pharmacy, Northwest A&F University, Yangling 712100, Shaanxi, PR China. Electronic address: jduan@nwafu.edu.cn.
PMID: 41740352 DOI: 10.1016/j.bioorg.2026.109657
Abstract

A series of 24 novel fluoroquinolone-uracil hybrids via various lengths linkers were designed, synthesized and evaluated for their Antibacterial activities against both Gram-negative and Gram-positive bacteria, including resistant strains. All target compounds were fully characterized by 1H NMR, 13C NMR and high-resolution mass spectrometry (HRMS). Most of the tested FQs-AU hybrids displayed a significant antipathogenic activity. For instance, A3, A4, A5, A9, A10, A11, B16, C19 and C22 demonstrated broad-spectrum Antibacterial activity against the 6 laboratory strains and 9 clinically isolated resistant strains, comparable to that of the reference Antibiotic ciprofloxacin. Especially, the A4 displayed enhanced activity against MDR MRSE 62 (0.125 μg/mL) compared to ciprofloxacin (1 μg/mL), potent antibiofilm activity (8 μg/mL), and excellent systemic safety in vitro (CC50 > 128 μg/mL and HC50 > 200 μg/mL) and in vivo (100 mg/mL). Additionally, in vivo results demonstrated that A4 effectively cleared MRSE 62 and promoted infected wound repair in a mouse model. The above findings highlight FQs-AU hybrids as a potential pharmacophore for the development of novel and more efficient antipathogenic agents.

Keywords

Antibacterial activity; Fluoroquinolone; Synthesis; Uracil.

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