Palestinian Medical and Pharmaceutical Journal (Pal. Med. Pharm. J.)

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Keywords

• Antimicrobial resistance
• Thiazolidine-4-One
• Molecular docking
• Computer-aided drug design
• Drug discovery
• Antimicrobial agents

Abstract

Several derivatives carrying thiazolidine-4-one pharmacophore were prepared to evaluate their antimicrobial activities. The set of compounds were shown to possess potential activities as determined by molecular docking studies for both candidal (14-alpha demethylase) and bacterial enzymes (Penicillin binding protein of E. coli). In vitro antimicrobial activities were also performed to confirm the molecular docking results. Molecular characterization by spectral techniques (FT-IR, 13C NMR and 1H NMR) was carried out to confirm the identity of the synthesized compounds. The synthesized compounds were evaluated for antibacterial and anticandidal activity by comparing them with the reference drugs (positive controls) ceftriaxone and fluconazole respectively. Four bacterial species (Klebsiella pneumonia, Escherichia coli, Staphylococcus epidermis, Staphylococcus aureus) and one fungal species (Candida albicans) were inoculated into petri dishes and were expose to the synthesized compounds by well diffusion method. The series of the proposed compounds were successfully synthesized and some of them were proven to have antibacterial activities comparable to the reference drug. Particularly, the compounds 2c and 2a posessed activities against K. pneumomia being higher than ceftriaxone with average inhibition zone diameters of 17 mm and 16 mm at highest concentration respectively. Compound 2b was effective against E. Coli also yielding higher activity than ceftriaxone achieving an average diameter of 17 mm at the highest concentration.

معلومات المقال

قيد النشر

الكلمات الإفتتاحية

• Antimicrobial resistance
• Thiazolidine-4-One
• Molecular docking
• Computer-aided drug design
• Drug discovery
• Antimicrobial agents

الملخص

Several derivatives carrying thiazolidine-4-one pharmacophore were prepared to evaluate their antimicrobial activities. The set of compounds were shown to possess potential activities as determined by molecular docking studies for both candidal (14-alpha demethylase) and bacterial enzymes (Penicillin binding protein of E. coli). In vitro antimicrobial activities were also performed to confirm the molecular docking results. Molecular characterization by spectral techniques (FT-IR, 13C NMR and 1H NMR) was carried out to confirm the identity of the synthesized compounds. The synthesized compounds were evaluated for antibacterial and anticandidal activity by comparing them with the reference drugs (positive controls) ceftriaxone and fluconazole respectively. Four bacterial species (Klebsiella pneumonia, Escherichia coli, Staphylococcus epidermis, Staphylococcus aureus) and one fungal species (Candida albicans) were inoculated into petri dishes and were expose to the synthesized compounds by well diffusion method. The series of the proposed compounds were successfully synthesized and some of them were proven to have antibacterial activities comparable to the reference drug. Particularly, the compounds 2c and 2a posessed activities against K. pneumomia being higher than ceftriaxone with average inhibition zone diameters of 17 mm and 16 mm at highest concentration respectively. Compound 2b was effective against E. Coli also yielding higher activity than ceftriaxone achieving an average diameter of 17 mm at the highest concentration.