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<p>To address the rise of multidrug-resistant bacteria by developing novel antibacterial agents with integrated capabilities for targeted delivery and real-time tracking, and to evaluate their potential for infection theranostics. Novel enaminonitrile-based pyridine and pyran derivatives were sustainably synthesized. Among them, lead compound 5 was assessed for in vitro DNA gyrase inhibition. Compound 5 was then radiolabeled with iodine-131, and radiolabeling yield was measured. In vivo biodistribution and pharmacokinetic profile were evaluated using an inflammatory murine model, with target-to-muscle ratios calculated. Compound 5 showed potent DNA gyrase inhibition (IC<sub>50</sub> = 11.31&#xa0;µg/mL). Radiolabeling produced [<sup>131</sup>I]I-5 with high radiolabeling yield (90.15%). In the murine model, the radiolabeled construct demonstrated rapid blood clearance and sustained, specific accumulation at the infection site, achieving a high target-to-muscle ratio of 5.18 at 1-h post-administration. This study introduces a new class of antibacterial agents and successfully translates a lead compound into a theranostic formulation. [<sup>131</sup>I]I-5 shows strong promise as a candidate for image-guided therapy and targeted treatment of infectious diseases.</p>

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Synthesis, 131I-radioiodination, and biodistribution of a novel nicotinonitrile derivative with in vitro antimicrobial and DNA gyrase inhibitory activities

  • 期刊论文

  • 发表日期：

    2026年7月17日

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  • Basant G. Salib,
  • Basma M. Essa,
  • Hesham A. Shamsel‐Din,
  • Mohamed A. Motaleb,
  • M. El-Tawoosy,
  • Adli A. Selim,
  • Sameh Ahmed Rizk,
  • Ahmed Hassan Ibrahim Faraag,
  • Mohamed A. Ali,
  • Islam Yousif Mostafa,
  • Reda Mansour,
  • Salah S. Elyan,
  • Mohamed Salah Basiouny,
  • Kurls E. Anwer

摘要

To address the rise of multidrug-resistant bacteria by developing novel antibacterial agents with integrated capabilities for targeted delivery and real-time tracking, and to evaluate their potential for infection theranostics. Novel enaminonitrile-based pyridine and pyran derivatives were sustainably synthesized. Among them, lead compound 5 was assessed for in vitro DNA gyrase inhibition. Compound 5 was then radiolabeled with iodine-131, and radiolabeling yield was measured. In vivo biodistribution and pharmacokinetic profile were evaluated using an inflammatory murine model, with target-to-muscle ratios calculated. Compound 5 showed potent DNA gyrase inhibition (IC50 = 11.31 µg/mL). Radiolabeling produced [131I]I-5 with high radiolabeling yield (90.15%). In the murine model, the radiolabeled construct demonstrated rapid blood clearance and sustained, specific accumulation at the infection site, achieving a high target-to-muscle ratio of 5.18 at 1-h post-administration. This study introduces a new class of antibacterial agents and successfully translates a lead compound into a theranostic formulation. [131I]I-5 shows strong promise as a candidate for image-guided therapy and targeted treatment of infectious diseases.