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<p>This study represents 6-(4-bromophenyl)-3-methyl-1-phenyl-1<i>H</i>-pyrazolo[3,4-<i>b</i>]pyridine-6-carbohydrazide’s (Br-hydrazide) in-vivo, in-vitro<i> anti</i>-bacterial, <i>anti</i>-diabetic, and theranostic potential. Docking showed binding energy of − 7.20&#xa0;kcal/mol, then Sulfaphenazole’s® − 6.00&#xa0;kcal/mol, against <i>S. aureus</i>, suggesting in-vivo toxicological evaluation. Br-hydrazide revealed enhanced in-vitro diabetic activity (IC<sub>50</sub> = 149.5&#xa0;μM) than Acarbose® (200.1&#xa0;μM) and bacterial activity showed (MIC: 5&#xa0;mg/mL; inhibition zone: 18&#xa0;mm) greater than Rifampicin® (15&#xa0;mm). The ∆G of − 5.70 and − 7.28&#xa0;kcal/mol compared well with Tracazolate®’s − 5.03, − 7.85&#xa0;kcal/mol for bacterial and diabetic potential. [<sup>99m</sup>Tc-Br-hydrazide], demonstrating ≥ 98 ± 0.5% RCP, 12&#xa0;h stability, and renal clearance in mice, showed potential for diagnostic purposes.</p> Graphical abstract <p></p>

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Synthesis, biological evaluation, and molecular docking of a bromo-hydrazide derivative as a bacterial targeting agent and its radiolabeling with technetium-99m for diagnostic applications

  • 期刊论文

  • 发表日期：

    2025年7月3日

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  • Iqra Rafique,
  • Saima Tariq,
  • Muhammad Saifullah,
  • Floris P. J. T. Rutjes,
  • Shakera Khatoon Rizvi

摘要

This study represents 6-(4-bromophenyl)-3-methyl-1-phenyl-1H-pyrazolo[3,4-b]pyridine-6-carbohydrazide’s (Br-hydrazide) in-vivo, in-vitro anti-bacterial, anti-diabetic, and theranostic potential. Docking showed binding energy of − 7.20 kcal/mol, then Sulfaphenazole’s® − 6.00 kcal/mol, against S. aureus, suggesting in-vivo toxicological evaluation. Br-hydrazide revealed enhanced in-vitro diabetic activity (IC50 = 149.5 μM) than Acarbose® (200.1 μM) and bacterial activity showed (MIC: 5 mg/mL; inhibition zone: 18 mm) greater than Rifampicin® (15 mm). The ∆G of − 5.70 and − 7.28 kcal/mol compared well with Tracazolate®’s − 5.03, − 7.85 kcal/mol for bacterial and diabetic potential. [99mTc-Br-hydrazide], demonstrating ≥ 98 ± 0.5% RCP, 12 h stability, and renal clearance in mice, showed potential for diagnostic purposes.

Graphical abstract