Novel Set of Highly Substituted Bis-pyridines: Synthesis, Molecular Docking and Drug-Resistant Antibacterial Profile

Author:

Kassab Refaie M1ORCID,A Zaki Magdi E2,Abo Dena Ahmed S34ORCID,Al-Hussain Sami A2,Abdel-Aziz Marwa M5,Muhammad Zeinab A3ORCID

Affiliation:

1. Department of Chemistry, Faculty of Science, Cairo University, Giza, 12613, Egypt

2. Department of Chemistry, Faculty of Science, Imam Mohammad Ibn Saud Islamic University (IMSIU), Riyadh, 11623, Saudi Arabia

3. Department of Pharmaceutical Chemistry, National Organization for Drug Control & Research (NODCAR), Giza, 12311, Egypt

4. Faculty of Oral & Dental Medicine, Future University in Egypt (FUE), New Cairo, 11865, Egypt

5. Regional Center for Mycology & Biotechnology, Al-Azhar University, Cairo, 11754, Egypt

Abstract

Aims: Development of antimicrobial agents having the ability to prevent bacterial biofilm formation which causes serious health problems, especially with antibiotic-resistant bacterial strains. Materials and methods: The use of 1,3-diaryl enones as structural motifs to access the pyridine core. Antimicrobial activities of the synthesized compounds against methicillin-susceptible Staphylococcus aureus, methicillin-resistant S. aureus and vancomycin-resistant S. aureus bacterial strains were investigated. Results: The newly synthesized bis-enones were used as building blocks to access some novel highly substituted bis-pyridine derivatives. Several novel bis-compounds showed great bacterial biofilm eradication activity. Conclusion: A new series of bis-chalcones was synthesized and their structural diversity was exploited to access the corresponding, more biologically active, pyridine core. These bis-pyridines showed respectable antibacterial activities against various drug-resistant bacterial strains: namely, methicillin-susceptible, methicillin-resistant and vancomycin-resistant S. aureus.

Publisher

Future Science Ltd

Subject

Drug Discovery,Pharmacology,Molecular Medicine

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