Synthesis, Characterization, and Exploring the Antibacterial and Antifungal Potential of 1,4-Dihydropyrimido[1,2-a]benzimidazole Derivatives

Objective: This study aims to synthesize and evaluate the antimicrobial efficacy of a series of 1,4-dihydropyrimido[1,2-a]benzimidazole derivatives (IVa–IVo) as potential therapeutic agents against antibiotic-resistant bacteria and fungi. The increasing prevalence of drug-resistant pathogens necessitates the discovery of novel antimicrobial compounds. Methods: The 1,4-dihydropyrimido[1,2-a]benzimidazole derivatives (IVa–IVo) were synthesized and characterized using various spectroscopic techniques. Their antimicrobial activity was assessed through the minimum inhibitory concentration (MIC) method against a spectrum of Gram-positive bacteria (Staphylococcus aureus, Streptococcus pyogenes), Gram-negative bacteria (Escherichia coli, Pseudomonas aeruginosa), and fungal strains (Candida albicans, Aspergillus niger, Aspergillus clavatus). Results and Discussion: Among the synthesized compounds, derivatives (IVj), (IVb), and (IVl) demonstrated significant antimicrobial activity, particularly against Staphylococcus aureus, Streptococcus pyogenes, and Escherichia coli, with MIC values comparable to those of standard antibiotics. While the overall activity of the 1,4-dihydropyrimido[1,2-a]benzimidazole derivatives was lower than that of the standard drugs, these compounds show promise as lead structures for further optimization and development in the quest to combat drug-resistant pathogens. Conclusions: The study successfully synthesized and identified 1,4-dihydropyrimido[1,2-a]benzimidazole derivatives with notable antimicrobial properties, especially against specific bacterial strains. These findings suggest that with further development, these compounds could contribute to the discovery of new antimicrobial agents to address the growing challenge of drug-resistant infections.

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Publication Details

Journal
Russian Journal of Bioorganic Chemistry
Published
2025-02-01
DOI
https://doi.org/10.1134/s1068162025010273
Citations
3
Primary Topic
Synthesis and biological activity
Type
article
Field-Weighted Citation Impact
2.81
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article

Synthesis, Characterization, and Exploring the Antibacterial and Antifungal Potential of 1,4-Dihydropyrimido[1,2-a]benzimidazole Derivatives

Dharmesh Katariya, Ketan Pancholi, Mahendra Borisagar
3 citations
Russian Journal of Bioorganic Chemistry
Synthesis and biological activity
2.81
article

Synthesis, Characterization, and Exploring the Antibacterial and Antifungal Potential of 1,4-Dihydropyrimido[1,2-a]benzimidazole Derivatives

Dharmesh Katariya, Ketan Pancholi, Mahendra Borisagar
article en
3 citations

Abstract

Objective: This study aims to synthesize and evaluate the antimicrobial efficacy of a series of 1,4-dihydropyrimido[1,2-a]benzimidazole derivatives (IVa–IVo) as potential therapeutic agents against antibiotic-resistant bacteria and fungi. The increasing prevalence of drug-resistant pathogens necessitates the discovery of novel antimicrobial compounds. Methods: The 1,4-dihydropyrimido[1,2-a]benzimidazole derivatives (IVa–IVo) were synthesized and characterized using various spectroscopic techniques. Their antimicrobial activity was assessed through the minimum inhibitory concentration (MIC) method against a spectrum of Gram-positive bacteria (Staphylococcus aureus, Streptococcus pyogenes), Gram-negative bacteria (Escherichia coli, Pseudomonas aeruginosa), and fungal strains (Candida albicans, Aspergillus niger, Aspergillus clavatus). Results and Discussion: Among the synthesized compounds, derivatives (IVj), (IVb), and (IVl) demonstrated significant antimicrobial activity, particularly against Staphylococcus aureus, Streptococcus pyogenes, and Escherichia coli, with MIC values comparable to those of standard antibiotics. While the overall activity of the 1,4-dihydropyrimido[1,2-a]benzimidazole derivatives was lower than that of the standard drugs, these compounds show promise as lead structures for further optimization and development in the quest to combat drug-resistant pathogens. Conclusions: The study successfully synthesized and identified 1,4-dihydropyrimido[1,2-a]benzimidazole derivatives with notable antimicrobial properties, especially against specific bacterial strains. These findings suggest that with further development, these compounds could contribute to the discovery of new antimicrobial agents to address the growing challenge of drug-resistant infections.

Russian Journal of Bioorganic ChemistryVol. 51(1)
Saurashtra University (IN), University of Kota (IN)
Zero hunger
Openalex Percentile: Top 12%
Synthesis and biological activity
2.81
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