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<p><i>Staphylococcus aureus</i> infections remain a major clinical challenge due to rapid acquisition of antimicrobial resistance, exemplified by Methicillin-Resistant <i>Staphylococcus aureus</i>. The imidazole scaffold has attracted sustained interest owing to its chemical versatility and broad pharmacological relevance. This review provides the first comprehensive and critical summary of recent advances in the synthesis and anti-staphylococcal activity of structurally diverse imidazole derivatives, including benzimidazoles, metal complexes, mercapto- and polycyclic analogues, and hybrid conjugates with bioactive motifs such as indole, berberine, and rifamycin. Both conventional and enabling methodologies (microwave- and ultrasound-assisted synthesis) are evaluated, with key transformations encompassing condensations, transition-metal-catalyzed couplings, complexation, El-Saghier, and Groebke–Blackburn–Bienaymé reactions. Structure–activity relationship analyses reveal that indole-, rifamycin-, berberine-, and N-aryl-substituted imidazoles exhibit superior potency against resistant strains, whereas hydroxynaphthalene, 2-phenyl-benzimidazole, imidazothiadiazole, and isatin analogues often show diminished activity. Collectively, these insights provide a rational framework for designing next-generation imidazole-based anti-staphylococcal agents, while underscoring the need for comprehensive profiling of stability, toxicity, and PK/PD properties to enable clinical translation.</p>

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Imidazole Scaffolds against Staphylococcus aureus and MRSA: a medicinal chemistry review

  • 期刊论文

  • 发表日期：

    2026年5月11日

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  • Supriyo Saha,
  • Muskan Singh,
  • Nikita Thapliyal,
  • Shakir Ahamad,
  • Shahnawaz Ali Bhat,
  • Vikash Jakhmola

摘要

Staphylococcus aureus infections remain a major clinical challenge due to rapid acquisition of antimicrobial resistance, exemplified by Methicillin-Resistant Staphylococcus aureus. The imidazole scaffold has attracted sustained interest owing to its chemical versatility and broad pharmacological relevance. This review provides the first comprehensive and critical summary of recent advances in the synthesis and anti-staphylococcal activity of structurally diverse imidazole derivatives, including benzimidazoles, metal complexes, mercapto- and polycyclic analogues, and hybrid conjugates with bioactive motifs such as indole, berberine, and rifamycin. Both conventional and enabling methodologies (microwave- and ultrasound-assisted synthesis) are evaluated, with key transformations encompassing condensations, transition-metal-catalyzed couplings, complexation, El-Saghier, and Groebke–Blackburn–Bienaymé reactions. Structure–activity relationship analyses reveal that indole-, rifamycin-, berberine-, and N-aryl-substituted imidazoles exhibit superior potency against resistant strains, whereas hydroxynaphthalene, 2-phenyl-benzimidazole, imidazothiadiazole, and isatin analogues often show diminished activity. Collectively, these insights provide a rational framework for designing next-generation imidazole-based anti-staphylococcal agents, while underscoring the need for comprehensive profiling of stability, toxicity, and PK/PD properties to enable clinical translation.