COMPARATIVE STUDY OF ANTIBACTERIAL ACTIVITY OF PYRAZINE–PIPERIDINE AMIDES AGAINST COMMON PATHOGENIC BACTERIA
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| Lingua: | inglese |
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Zenodo
2025
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| author | Kiruthiga Prakash1, Mohanraj Raja1, Mounishwaran Kamalesan1, Rameshkumar Neelamegam2, Kayalvizhi Nagarajan1* |
| author_facet | Kiruthiga Prakash1, Mohanraj Raja1, Mounishwaran Kamalesan1, Rameshkumar Neelamegam2, Kayalvizhi Nagarajan1* |
| contents | <p><span lang="EN-GB">The rising incidence of antibiotic-resistant bacterial infections underscores the urgent need for the development of innovative antibacterial agents that can surpass existing therapeutic constraints. Heterocyclic frameworks, especially those that incorporate pyrazine and piperidine pharmacophores, have demonstrated exceptional potential due to their improved biological compatibility and extensive pharmacological effects. In this research, a newly synthesized pyrazine–piperidine amide derivative was tested for its antibacterial efficacy against clinically significant Gram-positive (<em>Staphylococcus aureus, Bacillus subtilis</em>) and Gram-negative (<em>Escherichia coli, Klebsiella pneumoniae</em>) pathogens using the agar well diffusion method. This compound showed significant antibacterial activity that increased in a concentration-dependent fashion at 25, 50, 75, and 100 µg/mL. The highest level of inhibition was </span><span lang="EN-GB">observed for <em>S. aureus</em> (19.3 ± 0.5 mm) and <em>B. subtilis</em> (18.5 ±0.6 mm) at the maximum concentration, exceeding the inhibitory effect of the standard ciprofloxacin on <em>S. aureus</em>. The compound generated inhibition zones of 15.2 ± 0.3 mm (100 µg/mL) against <em>E. coli</em>, while <em>K. pneumoniae</em> exhibited a zone of inhibition of 13.8 ± 0.4 mm (100 µg/mL). In contrast, ciprofloxacin showed a ZOI of 14.3 ± 0.5 mm. Moderate yet encouraging inhibition was also noted against Gram-negative strains. The improved antimicrobial efficacy is attributed to synergistic structural attributes that facilitate better bacterial membrane penetration and enzyme interaction. Overall, the findings suggest that the synthesized pyrazine–piperidine amide derivative holds promise as an antibacterial lead compound, particularly against Gram-positive pathogens. Additional investigations involving MIC/MBC determination, analysis of mechanistic pathways, cytotoxicity assessment, and structural optimization are recommended to aid its advancement towards drug development.</span></p> |
| format | Recurso digital |
| id | zenodo_https___doi_org_10_5281_zenodo_17950646 |
| institution | Zenodo |
| language | eng |
| publishDate | 2025 |
| publisher | Zenodo |
| record_format | zenodo |
| spellingShingle | COMPARATIVE STUDY OF ANTIBACTERIAL ACTIVITY OF PYRAZINE–PIPERIDINE AMIDES AGAINST COMMON PATHOGENIC BACTERIA Kiruthiga Prakash1, Mohanraj Raja1, Mounishwaran Kamalesan1, Rameshkumar Neelamegam2, Kayalvizhi Nagarajan1* <p><span lang="EN-GB">The rising incidence of antibiotic-resistant bacterial infections underscores the urgent need for the development of innovative antibacterial agents that can surpass existing therapeutic constraints. Heterocyclic frameworks, especially those that incorporate pyrazine and piperidine pharmacophores, have demonstrated exceptional potential due to their improved biological compatibility and extensive pharmacological effects. In this research, a newly synthesized pyrazine–piperidine amide derivative was tested for its antibacterial efficacy against clinically significant Gram-positive (<em>Staphylococcus aureus, Bacillus subtilis</em>) and Gram-negative (<em>Escherichia coli, Klebsiella pneumoniae</em>) pathogens using the agar well diffusion method. This compound showed significant antibacterial activity that increased in a concentration-dependent fashion at 25, 50, 75, and 100 µg/mL. The highest level of inhibition was </span><span lang="EN-GB">observed for <em>S. aureus</em> (19.3 ± 0.5 mm) and <em>B. subtilis</em> (18.5 ±0.6 mm) at the maximum concentration, exceeding the inhibitory effect of the standard ciprofloxacin on <em>S. aureus</em>. The compound generated inhibition zones of 15.2 ± 0.3 mm (100 µg/mL) against <em>E. coli</em>, while <em>K. pneumoniae</em> exhibited a zone of inhibition of 13.8 ± 0.4 mm (100 µg/mL). In contrast, ciprofloxacin showed a ZOI of 14.3 ± 0.5 mm. Moderate yet encouraging inhibition was also noted against Gram-negative strains. The improved antimicrobial efficacy is attributed to synergistic structural attributes that facilitate better bacterial membrane penetration and enzyme interaction. Overall, the findings suggest that the synthesized pyrazine–piperidine amide derivative holds promise as an antibacterial lead compound, particularly against Gram-positive pathogens. Additional investigations involving MIC/MBC determination, analysis of mechanistic pathways, cytotoxicity assessment, and structural optimization are recommended to aid its advancement towards drug development.</span></p> |
| title | COMPARATIVE STUDY OF ANTIBACTERIAL ACTIVITY OF PYRAZINE–PIPERIDINE AMIDES AGAINST COMMON PATHOGENIC BACTERIA |
| url | https://doi.org/10.5281/zenodo.17950646 |