Antibacterial screening and molecular docking of 2-chloro/ nitrophenyl benzimidazole derivatives
The multidrug-resistant (MDR) bacteria have increased at an alarming rate and caused serious health problems throughout the world. The lack of newly introduced antibiotics prompts researchers to design and develop efficient antimicrobials to combat this issue. Application of benzimidazole as a pr...
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| Main Authors: | , , |
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| Format: | Proceeding Paper |
| Language: | English English |
| Published: |
Malaysian Institute of Chemistry (Institut Kimia Malaysia)
2023
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| Subjects: | |
| Online Access: | http://irep.iium.edu.my/105412/7/105412_Antibacterial%20screening%20and%20Molecular.pdf http://irep.iium.edu.my/105412/13/105412_Antibacterial%20screening%20and%20Molecular_SCOPUS.pdf http://irep.iium.edu.my/105412/ https://ikm.org.my/publications/malaysian-journal-of-chemistry/view-abstract.php?abs=J0044-ce74257 |
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| Summary: | The multidrug-resistant (MDR) bacteria have increased at an alarming rate and caused serious
health problems throughout the world. The lack of newly introduced antibiotics prompts researchers
to design and develop efficient antimicrobials to combat this issue. Application of benzimidazole
as a precursor in synthesis is one of many approaches to the discovery of new antibacterial
compounds. Fifteen benzimidazole derivatives bearing chlorophenyl and nitrophenyl groups
were screened using 96-well plate microdilution against eight bacteria strains; Bacillus cereus
(ATCC 11778), Streptococcus pyogenes (ATCC 19615), Staphylococcus aureus (ATCC 25923)
and Micrococcus luteus (IIUM), Escherichia coli (ATCC 25922), Pseudomonas aeruginosa
(ATCC 27853), Klebsiella pneumonia (ATCC 700603) and Salmonella typhimurium (IMR S
974/05 B). Norfloxacin was used as a positive control, incorporated with resazurin dye to indicate
bacterial growth. All compounds showed inhibition against Gram-positive and Gram-negative
bacteria albeit with low activity. Molecular docking of selected compounds was also conducted
to analyse their interactions with the protein targets of E.coli (PDB ID:4KFG) and S.aureus(PDB
ID:4URM). Most of the synthesised compounds showed better binding affinities than norfloxacin.
The solubility of the compounds in the in vitro analysis may contribute to the low antimicrobial
activity results. |
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