The recent advances in benzimidazole-based antimicrobials and antitubercular agents

Abstract Background Benzimidazole, a fused heterocyclic compound, has emerged as a privileged structure in medicinal chemistry due to its broad spectrum of biological activities, particularly in antimicrobial and antitubercular (anti-TB) applications. Its structural ingenuity allows for diverse substitutions at key positions, facilitating interactions with various biological targets such as bacterial enzymes and nucleic acids. Main body. Benzimidazole derivatives have demonstrated potent activity against a wide range of Gram-positive and Gram-negative bacteria, as well as against Mycobacterium tuberculosis , including drug-resistant strains. The pharmacophoric features of benzimidazole contribute to its ability to inhibit vital microbial processes, including cell wall synthesis, DNA replication, and energy metabolism. Structural optimization of benzimidazole scaffold has led to the development of several lead compounds with enhanced efficacy and pharmacokinetic profiles. Conclusion This review highlights the significance of benzimidazole as a privileged scaffold in the development of novel antimicrobial and anti-TB agents, emphasizing recent advances in structure–activity relationship (SAR) studies, and potential for future drug development.

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Publication Details

Journal
Future Journal of Pharmaceutical Sciences
Published
2025-08-15
DOI
https://doi.org/10.1186/s43094-025-00867-7
Citations
3
Primary Topic
Synthesis and biological activity
Type
article
Field-Weighted Citation Impact
2.81
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article

The recent advances in benzimidazole-based antimicrobials and antitubercular agents

Maiy Y. Jaballah, Nermin Samir, Eman Z. Elrazaz, Abdalrahman Tarek
3 citations
Future Journal of Pharmaceutical Sciences
Synthesis and biological activity
2.81
article

The recent advances in benzimidazole-based antimicrobials and antitubercular agents

Maiy Y. Jaballah, Nermin Samir, Eman Z. Elrazaz, Abdalrahman Tarek
article en
3 citations

Abstract

Abstract Background Benzimidazole, a fused heterocyclic compound, has emerged as a privileged structure in medicinal chemistry due to its broad spectrum of biological activities, particularly in antimicrobial and antitubercular (anti-TB) applications. Its structural ingenuity allows for diverse substitutions at key positions, facilitating interactions with various biological targets such as bacterial enzymes and nucleic acids. Main body. Benzimidazole derivatives have demonstrated potent activity against a wide range of Gram-positive and Gram-negative bacteria, as well as against Mycobacterium tuberculosis , including drug-resistant strains. The pharmacophoric features of benzimidazole contribute to its ability to inhibit vital microbial processes, including cell wall synthesis, DNA replication, and energy metabolism. Structural optimization of benzimidazole scaffold has led to the development of several lead compounds with enhanced efficacy and pharmacokinetic profiles. Conclusion This review highlights the significance of benzimidazole as a privileged scaffold in the development of novel antimicrobial and anti-TB agents, emphasizing recent advances in structure–activity relationship (SAR) studies, and potential for future drug development.

Future Journal of Pharmaceutical SciencesVol. 11(1)
Ain Shams University (EG)
Good health and well-being
Openalex Percentile: Top 9%
Synthesis and biological activity
2.81
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